NSC 185058

发表于2024年4月14日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

NSC 185058 纯度: 99.52%

NSC 185058 是一种 ATG4B 抑制剂。ATG4B 是一种主要的半胱氨酸蛋白酶 (cysteine protease)。NSC185058 抑制 ATG4B 从而显著减弱自噬 (autophagic) 活性。

NSC 185058 Chemical Structure

CAS No. : 39122-38-8

规格	价格	是否有货
5 mg	￥2300	In-stock
10 mg	￥3700	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

NSC 185058 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Autophagy Compound Library
Angiogenesis Related Compound Library
Targeted Diversity Library

生物活性

NSC 185058 is an inhibitor of ATG4B, a major cysteine protease. Inhibition of ATG4B using NSC 185058 markedly attenuates autophagic activity^[1].

IC₅₀ & Target

ATG4B^[1]
Autophagy^[1]

体内研究
(In Vivo)

NSC185058 is an ATG4B antagonist. ATG4B stimulates autophagy by promoting autophagosome formation through reversible modification of ATG8. Inclusion of the ATG4B inhibitor NSC185058 enhances the anti-tumor activity of radiation therapy (RT). NSC185058 decreases glioblastoma (GBM) cell tumorigenicity, and enhances the anti-tumor activity of RT when applied to orthotopic GBM xenograft models^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

215.27

Formula

C₁₁H₉N₃S

CAS 号

39122-38-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : ≥ 125 mg/mL (580.67 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.6453 mL	23.2266 mL	46.4533 mL
5 mM	0.9291 mL	4.6453 mL	9.2907 mL
10 mM	0.4645 mL	2.3227 mL	4.6453 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (9.66 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (9.66 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (9.66 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (9.66 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (9.66 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (9.66 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Huang T, et al. MST4 Phosphorylation of ATG4B Regulates Autophagic Activity, Tumorigenicity, and Radioresistance in Glioblastoma. Cancer Cell. 2017 Dec 11;32(6):840-855.e8.

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GANT 58(Synonyms: NSC 75503)

发表于2024年4月13日由上海金畔生物科技有限公司

GANT 58 (Synonyms: NSC 75503) 纯度: 99.91%

GANT 58 (NSC 75503) 是一种有效的 GLI 拮抗剂，抑制 GLI1 诱导的转录，IC₅₀ 为 5 μM。

GANT 58 Chemical Structure

CAS No. : 64048-12-0

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥563	In-stock
5 mg	￥512	In-stock
10 mg	￥818	In-stock
50 mg	￥2976	In-stock
100 mg	￥4800	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GANT 58 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Stem Cell Signaling Compound Library
Wnt/Hedgehog/Notch Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

GANT 58 (NSC 75503) is a potent GLI antagonist that inhibits GLI1-induced transcription with IC₅₀ of 5 μM^[1].

IC₅₀ & Target

IC50: 5 μM (Gli)^[1]

体外研究
(In Vitro)

GANT58 is a downstream inhibitor of Hh signaling. GANT58 is an indeed inhibitor of Hh signaling downstream of Smo and Sufu. GANT58 mainly acts at the nuclear level because transcription induced by GLI1 with a mutated nuclear export signal is still blocked. GANT58 efficiently inhibits in vitro tumor cell proliferation in a GLI-dependent manner and successfully blocks cell growth using human prostate cancer cells harboring downstream activation of the Hh pathway^[1]. GANT58 (NSC75503) has been shown to inhibit transcriptional activation by GLI1 (as well as by the other GLI species). GANT58 has been shown to inhibit GLI transactivation^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Nude mice are injected s.c. with GLI1-positive 22Rv1 prostate cancer cells, and tumors are established (median size ≈250 mm³). Nude mice are treated with daily s.c. injections at a concentration of 50 mg/kg of cyclopamine, GANT61, GANT58, or solvent only (n=4-5 for each group). However, after 3 days, cyclopamine-treated animals presented with severe ulcerations at the injection sites. Therefore, changing the treatment regimen to injections only every second day. To be able to compare all compounds, this protocol is also introduced for the GANTs, although mice treated with these compounds showed no such signs of toxicity. All injections are done 2-3 cm away from the tumors. During an 18-day treatment period, suppression of tumor cell growth is observed for all compounds. Treatment with cyclopamine or GANT58 results in the inhibition of additional xenograft growth and limited the increase in tumor size^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

392.48

Formula

C₂₄H₁₆N₄S

CAS 号

64048-12-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

Ethanol : 20 mg/mL (50.96 mM; Need ultrasonic)

DMSO : 9.09 mg/mL (23.16 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5479 mL	12.7395 mL	25.4790 mL
5 mM	0.5096 mL	2.5479 mL	5.0958 mL
10 mM	0.2548 mL	1.2740 mL	2.5479 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% saline

Solubility: 2 mg/mL (5.10 mM); Clear solution; Need ultrasonic

此方案可获得 2 mg/mL (5.10 mM) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% EtOH 90% (20% SBE-β-CD in saline)

Solubility: 2 mg/mL (5.10 mM); Clear solution; Need ultrasonic

此方案可获得 2 mg/mL (5.10 mM) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 0.91 mg/mL (2.32 mM); Clear solution

此方案可获得 ≥ 0.91 mg/mL (2.32 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 9.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
4.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 0.91 mg/mL (2.32 mM); Clear solution

此方案可获得 ≥ 0.91 mg/mL (2.32 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 9.1 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
5.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 0.91 mg/mL (2.32 mM); Clear solution

此方案可获得 ≥ 0.91 mg/mL (2.32 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 9.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Lauth M, et al. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8455-60.

[2]. Joo J, et al. GLI1 is a central mediator of EWS/FLI1 signaling in Ewing tumors. PLoS One. 2009 Oct 27;4(10):e7608.

Cell Assay ^[1]	HEK293 cells are transfected with GLI1 expression plasmid, together with the reporter plasmids 12× GliBS-Luc and R-Luc on 10 cm plates (day 0). Twenty-four hours later, cells are seeded in white 96 well plates with clear bottom at a density of 15,000 cells per well. Cells are allowed to attach, and compounds are added at a final concentration of 10 μM in DMSO (0.5% final DMSO concentration) (day 1.5). Cells are grown for another 24 h, subsequently lysed, and then analyzed by using the Dual Luciferase kit. Plates are read on a Berthold Technologies microplate luminometer. Subconfluent cells are grown in reduced FBS (2.5%) for 48 h in the presence of 5 μM test compound (or DMSO) on white 96 well plates with clear bottom. Subsequently, cells are labeled for 2 h with BrdU, fixed, and analyzed. Samples are read on a Molecular Devices SpectraMax Gemini EM^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] 5×10⁶ 22Rv1 cells are suspended in a total volume of 100 μL of a 1:1 mixture of RPMI medium 1640:Matrigel (E1270). The cell suspension is injected s.c. at the posterior flank of female BALB/c nude mice (nu/nu). Tumors are grown until they reached a median size of ≈250 mm³ (5-6 days). Animals are randomly divided into four groups (n=4-5) and treated with solvent only (corn oil:ethanol, 4:1) or compounds in solvent (50 mg/kg) for 16 days s.c. injections of compounds are performed several centimeters away from the tumor. Tumor volumes are calculated by the formula length×width×0.5×(length+width). At the end of the treatment period, animals are given a BrdU pulse (50 mg/kg) for 30 min, and tumors are removed. All animal experiments are approved by local ethics authorities. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Lauth M, et al. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8455-60. [2]. Joo J, et al. GLI1 is a central mediator of EWS/FLI1 signaling in Ewing tumors. PLoS One. 2009 Oct 27;4(10):e7608.

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NSC 601980 (analog)

发表于2024年4月13日由上海金畔生物科技有限公司

NSC 601980 (analog) 纯度: ≥98.0%

NSC 601980 analog 是 NSC601980 的类似物，NSC 601980 在酵母筛选实验结果中，表现出了抗肿瘤活性, 能够在 COLO 205 和 HT29 细胞株里很好的抑制细胞增殖，Log GI 50 分别是-6.6 和 -6.9。

NSC 601980 (analog) Chemical Structure

CAS No. : 91757-46-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1760	In-stock
5 mg	￥1600	In-stock
10 mg	￥2400	In-stock
50 mg	￥7000	In-stock
100 mg	￥11000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

NSC 601980 (analog) 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Cancer Compound Library

生物活性

NSC 601980 analog is the analog of the NSC601980, NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.

分子量

250.30

Formula

C₁₅H₁₄N₄

CAS 号

91757-46-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 30 mg/mL (119.86 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.9952 mL	19.9760 mL	39.9521 mL
5 mM	0.7990 mL	3.9952 mL	7.9904 mL
10 mM	0.3995 mL	1.9976 mL	3.9952 mL

参考文献

[1]. Parkanyi Cyril, et al. Convenient synthesis of arylazo derivatives of quinoxaline, 1,4-benzothiazine, and 1,4-benzoxazine. From Journal of Heterocyclic Chemistry (1984), 21(2), 521-4.

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NSC 601980

发表于2024年4月13日由上海金畔生物科技有限公司

NSC 601980 纯度: 98.11%

NSC 601980 酵母筛选实验结果中，表现出了抗肿瘤活性, 能够在COLO 205 and HT29细胞株里很好的抑制细胞增殖，Log GI 50分别是-6.6和 -6.9。

NSC 601980 Chemical Structure

CAS No. : 2070018-27-6

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1760	In-stock
5 mg	￥1600	In-stock
10 mg	￥2400	In-stock
50 mg	￥7000	In-stock
100 mg	￥11000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

NSC 601980 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Cancer Compound Library

生物活性

NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.

分子量

248.28

Formula

C₁₅H₁₂N₄

CAS 号

2070018-27-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 25 mg/mL (100.69 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.0277 mL	20.1386 mL	40.2771 mL
5 mM	0.8055 mL	4.0277 mL	8.0554 mL
10 mM	0.4028 mL	2.0139 mL	4.0277 mL

参考文献

[1]. DTP Datawarehouse Index Results.

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L-Alanosine(Synonyms: 丙氨菌素; NSC-153353; SDX-102)

发表于2024年4月12日由上海金畔生物科技有限公司

L-Alanosine (Synonyms: 丙氨菌素; NSC-153353; SDX-102) 纯度: ≥95.0%

L-Alanosine (NSC-153353) 是来自 Streptomyces alanosinicus 的抗生素，具有抗肿瘤和抗病毒活性。L-Alanosine (NSC-153353) 抑制腺苷酸琥珀酸合成酶，将肌苷一磷酸 (IMP) 转化为腺苷酸琥珀酸。L-Alanosine (NSC-153353) 阻断常见的从头嘌呤生物合成途径，从而抑制具有 MTAP 缺陷的肿瘤细胞。

L-Alanosine Chemical Structure

CAS No. : 5854-93-3

规格	价格	是否有货
1 mg	￥1150	In-stock
5 mg	￥3400	In-stock
10 mg	￥5800	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

L-Alanosine 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus

生物活性

L-Alanosine (NSC-153353), an antibiotic from Streptomyces alanosinicus, has antineoplastic activity. L-Alanosine (NSC-153353) inhibits adenylosuccinate synthetase, which converts inosine monophospate (IMP) into adenylosuccinate. L-Alanosine (NSC-153353) blocks the common de novo purine biosynthesis pathway and, thereby, inhibits tumor cells with MTAP deficiency^[1]^[2]^[3].

Clinical Trial

分子量

149.11

Formula

C₃H₇N₃O₄

CAS 号

5854-93-3

中文名称

丙氨菌素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

溶解性数据

In Vitro:

H₂O : 15 mg/mL (100.60 mM; ultrasonic and adjust pH to 8 with NaOH)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	6.7065 mL	33.5323 mL	67.0646 mL
5 mM	1.3413 mL	6.7065 mL	13.4129 mL
10 mM	0.6706 mL	3.3532 mL	6.7065 mL

请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

参考文献

[1]. Efferth T, et al. Identification of gene expression profiles predicting tumor cell response to L-alanosine. Biochem Pharmacol. 2003 Aug 15;66(4):613-21.

[2]. Chitnis MP, et al. Antitumor effect of L-alanosine (NSC 153553) on sensitive and resistant sublines of murine leukemias. Tumori. 1984 Aug 31;70(4):317-20.

[3]. Tyagi AK, et al. Identification of the antimetabolite of L-alanosine, L-alanosyl-5-amino-4-imidazolecarboxylic acid ribonucleotide, in tumors and assessment of its inhibition of adenylosuccinate synthetase. Cancer Res. 1980 Dec;40(12):4390-7.

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NSC 88911-d3(Synonyms: Oestrone methyl ether-d3; 3-O-Methylestrone-d3)

发表于2024年4月12日由上海金畔生物科技有限公司

NSC 88911-d3 (Synonyms: Oestrone methyl ether-d3; 3-O-Methylestrone-d3)

NSC 88911-d3 Chemical Structure

CAS No. : 1093230-99-9

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分子量	287.41
Formula	C₁₉H₂₁D₃O₂
CAS 号	1093230-99-9
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.

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Lomustine(Synonyms: 洛莫司汀; CCNU; NSC 79037)

发表于2024年4月12日由上海金畔生物科技有限公司

Lomustine (Synonyms: 洛莫司汀; CCNU; NSC 79037) 纯度: 99.91%

Lomustine (CCNU; NSC 79037) 是一种 DNA 烷化剂 (DNA alkylator)，具有抗肿瘤活性。

Lomustine Chemical Structure

CAS No. : 13010-47-4

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Free Sample (0.1-0.5 mg)		Apply now
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生物活性

Lomustine (CCNU; NSC 79037) is a DNA alkylating agent, with antitumor activity.

IC₅₀ & Target

DNA Alkylator^[1]

体外研究
(In Vitro)

Lomustine (CCNU; NSC 79037) is a DNA alkylating agent. Lomustine (CCNU, 0-250 μM) is cytotoxic to the U87-MG cells expressing tumor-derived mutant IDH1, and has little effect on the expression of wild-type IDH1. The combination of Lomustine and procarbazine or vincristine has no additive effect on the killing of cells expressing mutant or wild-type IDH1. Moreover, overexpression of either ALKBH2 or ALKBH3 partially reduces the death HT1080 cells exposed to Lomustine^[1]. Lomustine (CCNU) suppresses U87-MG growth with an ED50 of 68.1 μM. Lomustine (CCNU) (30, 40 μM) in combination with docosahexaenoic acid (DHA) darmatically inhibits 2 additional human-derived glioblastoma cell lines, and induces U87-MG apoptosis and necrosis. Lomustine (30 μM) causes G2/M arrest^[2]. Lomustine (CCNU) reduces the viability of F98 rat orthotopic glioma cells and Tu-2449 mouse glioma cell line, with IC₅₀s of 20.8 µM and 18.6 µM, respectively^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Lomustine (CCNU; NSC 79037) (30 mg/kg) in combination with Toca 511 + 5-FC prolongs survival in rats bearing F98 tumor cells. Lomustine (CCNU) (30 mg/kg) combined with Toca-511 + 5-FC also exhibits antitumor activity in the B6C3F1 mice bearing Tu-2449 glioma cells^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

233.70

Formula

C₉H₁₆ClN₃O₂

CAS 号

13010-47-4

中文名称

洛莫司汀；氯乙环已亚硝脲

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (427.90 mM)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.2790 mL	21.3950 mL	42.7899 mL
5 mM	0.8558 mL	4.2790 mL	8.5580 mL
10 mM	0.4279 mL	2.1395 mL	4.2790 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (10.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.70 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (10.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.70 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (10.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.70 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Wang P, et al. Oncometabolite D-2-Hydroxyglutarate Inhibits ALKBH DNA Repair Enzymes and Sensitizes IDH Mutant Cells to Alkylating Agents. Cell Rep. 2015 Dec 22;13(11):2353-2361.

[2]. Harvey KA, et al. Enhanced anticancer properties of lomustine in conjunction with docosahexaenoic acid in glioblastoma cell lines. J Neurosurg. 2015 Mar;122(3):547-56.

[3]. Yagiz K, et al. Toca 511 plus 5-fluorocytosine in combination with lomustine shows chemotoxic and immunotherapeutic activity with no additive toxicity in rodent glioblastoma models. Neuro Oncol. 2016 Oct;18(10):1390-401.

Cell Assay ^[2]	Initially, cells (5000 cells/well) are cultured in 96-well flat-bottom plates overnight in complete medium to establish a linear growth rate. Spent medium is replaced with new medium supplemented with 2% FBS and varying treatments (100 μL total volume/well). Ethanol-supplemented cells (< 0.5%) serve as the vehicle control. Cells are maintained at 37°C in 5% CO₂ in a humidified atmosphere for 24 hours prior to assessment of cell growth with the WST-1 assay reagent. Medium alone combined with the WST-1 assay reagent establishes nonspecific values that are subtracted from the experimental optical density (OD) readings (OD at 450 nm). Vehicle control OD readings serve as standard proliferative potential normalized to 100%. The proliferation index is calculated by dividing the average OD treatment reading by the average OD vehicle reading and multiplying by 100^[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] Groups of B6C3F1 mice receive PBS or 5-FC only as a control during the study (n = 8 per group). One group of mice (Lomustine Day 1 + PBS) receive one dose of Lomustine (30 mg/kg) on day 1 and a total of six cycles of PBS (800 μL/day, BID for 4 consecutive days every 10 days). The rest of the mice receive 5-FC (500 mg/kg/dose, IP, BID) for 4 consecutive days, plus Lomustine at day 1 (Lomustine (CCNU) Day 1 + 5-FC) or day 43 (Lomustine (CCNU) Day 43 + 5-FC). Cycles of 4-days on, 10-days off 5-FC or PBS are repeated a total of 6 times. Each experiment is terminated at the end of the last 5-FC treatment. All tissues are collected and saved for histopathology. Toxicity in groups receiving Lomustine is compared to the groups receiving PBS or 5-FC alone or in combination with 5-FC at designated time points^[3]. Rats^[3] Groups of rats receive PBS or 5-FC only as controls during the study (n = 8 per group). One group of rats (Lomustine (CCNU) Day 1 + PBS) receive one dose of Lomustine (30 mg/kg) at day 1 and a total of six cycles of PBS (8 mL/day, BID). The rest of the rats receive 5-FC (500 mg/kg/dose, IP, BID) for 5 consecutive days, followed by 2 days off drug, plus Lomustine on day 1 (Lomustine (CCNU) Day 1 + 5-FC) or day 22 (Lomustine (CCNU) Day 22 + 5-FC). Cycles of 5-days on, 2-days off 5-FC or PBS are repeated a total of 6 times^[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Wang P, et al. Oncometabolite D-2-Hydroxyglutarate Inhibits ALKBH DNA Repair Enzymes and Sensitizes IDH Mutant Cells to Alkylating Agents. Cell Rep. 2015 Dec 22;13(11):2353-2361. [2]. Harvey KA, et al. Enhanced anticancer properties of lomustine in conjunction with docosahexaenoic acid in glioblastoma cell lines. J Neurosurg. 2015 Mar;122(3):547-56. [3]. Yagiz K, et al. Toca 511 plus 5-fluorocytosine in combination with lomustine shows chemotoxic and immunotherapeutic activity with no additive toxicity in rodent glioblastoma models. Neuro Oncol. 2016 Oct;18(10):1390-401.

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Merbarone(Synonyms: NSC 336628)

发表于2024年4月12日由上海金畔生物科技有限公司

Merbarone (Synonyms: NSC 336628) 纯度: 99.49%

Merbarone (NSC 336628) 是一种具有口服活性的拓扑异构酶 II (topoisomerase II) 抑制剂。Merbarone 的主要作用是阻断拓扑异构酶 II 介导的 DNA 切割，而不会稳定拓扑 II-DNA 共价复合物。Merbarone 具有抗肿瘤功效。

Merbarone Chemical Structure

CAS No. : 97534-21-9

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生物活性

Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent^[1]^[2]^[4].

IC₅₀ & Target

topoisomerase II^[1]

体外研究
(In Vitro)

Merbarone (1-100 μM) inhibits L1210 cells proliferation in a concentration-dependent manner, with an IC₅₀ of 10 μM^[3].
Merbarone (10-200 μM; 10 min) inhibits DNA relaxation catalyzed by human topoisomerase IIα, with an IC₅₀ of ∼40 μM^[1].
Merbarone (25-200 μM; 6 min) blocks tyopoisomerase II-mediated DNA cleavage, with an IC₅₀ of ∼50 μM^[1].
Merbarone (100 μM; 6 min) inhibits topoisomerase II-mediated DNA cleavage in a global manner^[1].
Merbarone (100 μM; 6 min) does not impair topoisomerase II•DNA binding^[1].
Merbarone (200 μM; 4-16 min) does not inhibit topoisomerase II-catalyzed ATP hydrolysis^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Merbarone (50 mg/kg; daily i.p. for 5 d) achieves a maximum increased life span (ILS) of 101% in P388 murine leukemia^[2].
Merbarone (124 mg/kg; daily p.o. for 9 d) has anti-tumor activity in mice^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

263.27

Formula

C₁₁H₉N₃O₃S

CAS 号

97534-21-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (237.40 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7984 mL	18.9919 mL	37.9838 mL
5 mM	0.7597 mL	3.7984 mL	7.5968 mL
10 mM	0.3798 mL	1.8992 mL	3.7984 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: 2.5 mg/mL (9.50 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (9.50 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (9.50 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (9.50 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Fortune JM, et, al. Merbarone inhibits the catalytic activity of human topoisomerase IIalpha by blocking DNA cleavage. J Biol Chem. 1998 Jul 10;273(28):17643-50.

[2]. Brewer AD, et, al. 5-(N-phenylcarboxamido)-2-thiobarbituric acid (NSC 336628), a novel potential antitumor agent. Biochem Pharmacol. 1985 Jun 1;34(11):2047-50.

[3]. Cooney DA, et, al. Initial mechanistic studies with merbarone (NSC 336628). Biochem Pharmacol. 1985 Sep 15;34(18):3395-8.

[4]. Chen M, et, al. Differences in inhibition of chromosome separation and G2 arrest by DNA topoisomerase II inhibitors merbarone and VM-26. Cancer Res. 1995 Apr 1;55(7):1509-16.

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NSC 405020

发表于2024年4月11日由上海金畔生物科技有限公司

NSC 405020 纯度: 99.75%

NSC 405020 是MT1-MMP抑制剂，能特异地靶向MT1-MMP的PEX结构域，不会抑制MT1-MMP和MMP-2的催化活性。

NSC 405020 Chemical Structure

CAS No. : 7497-07-6

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Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥785	In-stock
10 mg	￥714	In-stock
50 mg	￥2727	In-stock
100 mg		询价
200 mg		询价

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NSC 405020 相关产品

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生物活性

NSC 405020 is a novel small molecule inhibitor of MT1-MMP that specifically targets PEX domain rather than the catalytic domain of MT1-MMP with IC50 >100 μM and does not inhibit the catalytic activity of MT1-MMP or MMP-2. IC50 value: > 100 uM [1] Target: MT1-MMP PEX inhibitor NSC-405020 directly interacts with and binds to PEX in a vicinity of Met-328, Arg-330, Asp-376, Met-22 and Ser-470 of the druggable pocket in the full-length MT1-MMP structure, which affects the conformation and flexibility of blades I to IV of the β-propeller resulting in the decrease of the PEX-dependent homodimerization of cellular MT1-MMP. NSC-405020 dose not affect the ability of MT1-MMP to activate MMP-2 but its ability to degrade COL-I.

分子量

260.16

Formula

C₁₂H₁₅Cl₂NO

CAS 号

7497-07-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 260 mg/mL (999.38 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.8438 mL	19.2189 mL	38.4379 mL
5 mM	0.7688 mL	3.8438 mL	7.6876 mL
10 mM	0.3844 mL	1.9219 mL	3.8438 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (9.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.61 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Remacle AG, et al. Novel MT1-MMP small-molecule inhibitors based on insights into hemopexin domain function in tumor growth. Cancer Res. 2012 May 1;72(9):2339-49.

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Treosulfan(Synonyms: NSC 39069; Treosulphan)

发表于2024年4月11日由上海金畔生物科技有限公司

Treosulfan (Synonyms: NSC 39069; Treosulphan) 纯度: ≥98.0%

Treosulfan (NSC 39069) 是一种双功能的烷化剂 (alkylator)，对卵巢癌及其他的实体瘤都有抑制效果。

Treosulfan Chemical Structure

CAS No. : 299-75-2

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥940	In-stock
5 mg	￥850	In-stock
10 mg	￥1400	In-stock
50 mg	￥5500	In-stock
100 mg	￥9500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

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FDA Approved & Pharmacopeial Drug Library
Anti-Lung Cancer Compound Library
Tumorigenesis Related Compound Library
Rare Diseases Drug Library

生物活性

Treosulfan (NSC 39069) is a bifunctional alkylating agent with activity in ovarian cancer and other solid tumor types.

IC₅₀ & Target

DNA Alkylator^[1]

体外研究
(In Vitro)

Treosulfan is an alkylating agent. Treosulfan inhibits several cancer cell lines, such as Panc-1, Miapaca-2 and Capan-2 cells, with IC₅₀s of 3.6 μg/mL, 1.8 μg/mL and 2.1 μg/mL respectively, and shows nearly 100% cytotoxicity on these cell lines at 100 μg/mL. Treosulfan (0.1-100 μg/mL) in combination with LY 188011 exhibits enhanced activity against cancer cells. However, Treosulfan (1, 2.5, 5 μg/ml) combined with 5-FU (0.1, 0.25, 0.5 μg/ml) has antagonistic effect on Panc-1 cells at intermediate and high concentrations, and on Miapaca-2 cells at all doses^[1]. Treosulfan (800 µg/mL) dramatically reduces erythrocyte forward scatter, increases the percentage of annexin-V-binding cells, [Ca²⁺]_i, and ROS. Removal of extracellular Ca²⁺ abrogates the effect of Treosulfan on annexin-V-binding^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Treosulfan (1.5 g/kg/day) induces a rapid myeloablation, depletes the splenic B and T cells in mice. Treosulfan (1.5 g/kg/day) causes olny interleukin-2 production in spleen cells for a short time and without obvious significant effect on synthesis of tumor necrosis factor-α and/or IFN-γ in mice^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

278.30

Formula

C₆H₁₄O₈S₂

CAS 号

299-75-2

中文名称

曲奥舒凡

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (359.32 mM)

H₂O : 50 mg/mL (179.66 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.5932 mL	17.9662 mL	35.9324 mL
5 mM	0.7186 mL	3.5932 mL	7.1865 mL
10 mM	0.3593 mL	1.7966 mL	3.5932 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (8.98 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.98 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (8.98 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.98 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (8.98 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Nitsch E, et al. Synergistic cytotoxic activity of treosulfan and LY 188011 in pancreatic cancer cell lines. Anticancer Res. 2014 Apr;34(4):1779-84.

[2]. Peter T, et al. Programmed erythrocyte death following in vitro Treosulfan treatment. Cell Physiol Biochem. 2015;35(4):1372-80.

[3]. Sjöö F, et al. Myeloablative and immunosuppressive properties of treosulfan in mice. Exp Hematol. 2006 Jan;34(1):115-21.

Cell Assay ^[1]	For cytotoxicity assays, the cells are plated at 1×10⁴ cells/mL grown in 100 μL volume per well of 96-well tissue culture plates. The cells are left to adhere overnight and thereafter incubated with different concentrations of Treosulfan alone or in combination with LY 188011. The drug combination is added to the cell cultures simultaneously or sequentially (the second drug added 12 h after the first). After 72 h of incubation, Alamar Blue® solution is added to the wells prior to further overnight incubation. Absorbance is then measured on a spectrophotometer and cell proliferation and cytotoxicity of drugs are calculated. In some experiments, proliferation and cytotoxicity are also determined by using trypan blue exclusion and cell counting with an improved Neubauer hemocytometer and cell viability assessed by staining the cells with 7-amino-actinomycin D (final concentration 200 μg/mL) and Annexin-V and analyzing via flow cytometry using a FACS Scan flow cytometer^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] Female BALB/c mice are 10 to 12 weeks old and weighed approximately 20 g. Animals are fed with standard pelleted food and water ad libitum. They are housed in a climatized chamber with a dark/light cycle of 12 hours. They are divided into four groups: one group is given Treosulfan (1.5 g/kg/day) for 3 consecutive days, one group receives NSC-26271 (0.1 g/kg/day) for 2 consecutive days, one group is treated with liposomal NCI C01592 (37 mg/kg/day) for 4 consecutive days, and there is a control group with no treatment. NSC-26271, NCI C01592, and Treosulfan doses are given at sublethal doses to maintain survival of the animals without bone marrow support. Animals are sacrificed on days 1, 3, 6, 9, and 12, after the last dose of treatment, and the spleen and femurs are removed. Six animals are included in each time point for the treated animals and two control animals^[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Nitsch E, et al. Synergistic cytotoxic activity of treosulfan and LY 188011 in pancreatic cancer cell lines. Anticancer Res. 2014 Apr;34(4):1779-84. [2]. Peter T, et al. Programmed erythrocyte death following in vitro Treosulfan treatment. Cell Physiol Biochem. 2015;35(4):1372-80. [3]. Sjöö F, et al. Myeloablative and immunosuppressive properties of treosulfan in mice. Exp Hematol. 2006 Jan;34(1):115-21.

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NSC 95397

发表于2024年3月20日由上海金畔生物科技有限公司

NSC 95397 纯度: ≥99.0%

NSC 95397 是一种有效选择性的 Cdc25 双特异性磷酸酶抑制剂 (Cdc25A、Cdc25B 以及 Cdc25C 的 K_i 值分别为 32、96、40 nM，人亚型 Cdc25A、人亚型 Cdc25C 以及 Cdc25B 的 IC₅₀ 值分别为 22.3、56.9、125 nM)。NSC 95397 抑制丝裂原活化蛋白激酶磷酸酶-1 (MKP-1)，并通过 MKP-1 和 ERK1/2 途径抑制结肠癌细胞的增殖并诱导细胞凋亡。

NSC 95397 Chemical Structure

CAS No. : 93718-83-3

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1024	In-stock
5 mg	￥1500	In-stock
10 mg	￥2200	In-stock
25 mg	￥5000	In-stock
50 mg	￥9000	In-stock
100 mg		询价

* Please select Quantity before adding items.

NSC 95397 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Kinase Inhibitor Library
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Phosphatase Inhibitor Library
Anti-Colorectal Cancer Compound Library

生物活性

NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (K_i=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC₅₀=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B))^[1]. NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway^[2].

IC₅₀ & Target

Ki: 32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C)^[1]
IC50: 22.3 nM (human Cdc25A) , 56.9 nM (human Cdc25C), 125 nM (Cdc25B)^[1]

体外研究
(In Vitro)

NSC 95397 (0, 10, and 20 µM; 24 hour) decreases the cell viability of three colon cancer cell lines SW480, SW620, and DLD-1 in a concentration-dependent manner^[2].
NSC 95397(10 μM; 24 hour) upregulates p21 while downregulates CDK4 and CDK6 were d in all three colon cancer cell lines SW480, SW620, and DLD-1 cells^[2].
NSC 95397 (10 μM; 24 hour) reduces the phosphorylation of retinoblastoma protein (Rb) on Ser795 and Ser807/811^[2].
NSC 95397 (20 μM; 24 hours) significantly increases cleaved caspase-9, -3, -7 and PARP levels^[2].
NSC 95397 (10 μM; 6 hours) enhances the phosphorylation of its downstream ERK1/2 at Thr202/Tyr 204^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:	Human colon cancer cell lines, SW480, SW620, and DLD-1
Concentration:	0, 10, and 20 µM
Incubation Time:	24 hours
Result:	The IC₅₀ values of NSC 95397 for the cell growth of SW480, SW620, and DLD-1 cells were 9.9, 14.1 and 18.6 μM, respectively.

Western Blot Analysis^[2]

Cell Line:	SW480, SW620, and DLD-1 cells
Concentration:	10 μM
Incubation Time:	24 hours
Result:	p21 was upregulated while CDK4 and CDK6 were downregulated. Rduced the phosphorylation of Rb on Ser795 and Ser807/811

分子量

310.39

Formula

C₁₄H₁₄O₄S₂

CAS 号

93718-83-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (322.18 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2218 mL	16.1088 mL	32.2175 mL
5 mM	0.6444 mL	3.2218 mL	6.4435 mL
10 mM	0.3222 mL	1.6109 mL	3.2218 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 10 mg/mL (32.22 mM); Clear solution

此方案可获得 ≥ 10 mg/mL (32.22 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 10 mg/mL (32.22 mM); Clear solution

此方案可获得 ≥ 10 mg/mL (32.22 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在 MCE 网站选购。

参考文献

[1]. Lazo JS, et al. Identification of a potent and selective pharmacophore for Cdc25 dual specificity phosphatase inhibitors. Mol Pharmacol. 2002 Apr;61(4):720-8.

[2]. Dubey NK, et al. NSC 95397 Suppresses Proliferation and Induces Apoptosis in Colon Cancer Cells through MKP-1 and the ERK1/2 Pathway. Int J Mol Sci. 2018 May 31;19(6). pii: E1625.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

NSC 95397

发表于2024年3月20日由上海金畔生物科技有限公司

NSC 95397 纯度: ≥99.0%

NSC 95397 Chemical Structure

CAS No. : 93718-83-3

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1024	In-stock
5 mg	￥1500	In-stock
10 mg	￥2200	In-stock
25 mg	￥5000	In-stock
50 mg	￥9000	In-stock
100 mg		询价

* Please select Quantity before adding items.

NSC 95397 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Kinase Inhibitor Library
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Phosphatase Inhibitor Library
Anti-Colorectal Cancer Compound Library

生物活性

IC₅₀ & Target

Ki: 32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C)^[1]
IC50: 22.3 nM (human Cdc25A) , 56.9 nM (human Cdc25C), 125 nM (Cdc25B)^[1]

体外研究
(In Vitro)

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:	Human colon cancer cell lines, SW480, SW620, and DLD-1
Concentration:	0, 10, and 20 µM
Incubation Time:	24 hours
Result:	The IC₅₀ values of NSC 95397 for the cell growth of SW480, SW620, and DLD-1 cells were 9.9, 14.1 and 18.6 μM, respectively.

Western Blot Analysis^[2]

Cell Line:	SW480, SW620, and DLD-1 cells
Concentration:	10 μM
Incubation Time:	24 hours
Result:	p21 was upregulated while CDK4 and CDK6 were downregulated. Rduced the phosphorylation of Rb on Ser795 and Ser807/811

分子量

310.39

Formula

C₁₄H₁₄O₄S₂

CAS 号

93718-83-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (322.18 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2218 mL	16.1088 mL	32.2175 mL
5 mM	0.6444 mL	3.2218 mL	6.4435 mL
10 mM	0.3222 mL	1.6109 mL	3.2218 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 10 mg/mL (32.22 mM); Clear solution

此方案可获得 ≥ 10 mg/mL (32.22 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 10 mg/mL (32.22 mM); Clear solution

此方案可获得 ≥ 10 mg/mL (32.22 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Lazo JS, et al. Identification of a potent and selective pharmacophore for Cdc25 dual specificity phosphatase inhibitors. Mol Pharmacol. 2002 Apr;61(4):720-8.

[2]. Dubey NK, et al. NSC 95397 Suppresses Proliferation and Induces Apoptosis in Colon Cancer Cells through MKP-1 and the ERK1/2 Pathway. Int J Mol Sci. 2018 May 31;19(6). pii: E1625.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

NSC697923

发表于2024年3月20日由上海金畔生物科技有限公司

NSC697923 纯度: ≥97.0%

NSC697923 是一种有效的 UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) 抑制剂。NSC697923 通过促进 p53 野生型神经母细胞瘤细胞中 p53 的核输入而诱导神经母细胞瘤细胞死亡。NSC697923 通过激活 JNK 介导的凋亡途径诱导 p53 突变神经母细胞瘤细胞死亡。NSC697923 抑制 DNA 损伤和 NF-κB 信号传导。具有抗肿瘤活性。

NSC697923 Chemical Structure

CAS No. : 343351-67-7

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
5 mg	￥500	In-stock
10 mg	￥800	In-stock
25 mg	￥1500	In-stock
50 mg	￥2500	In-stock
100 mg	￥4000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

NSC697923 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Metabolism/Protease Compound Library
NF-κB Signaling Compound Library
Anti-Cancer Compound Library
Oxygen Sensing Compound Library
Ubiquitination Compound Library
Anti-Liver Cancer Compound Library

生物活性

NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity^[1]^[2].

体外研究
(In Vitro)

NSC697923 (0-5 μM; 24 hours) shows cytotoxic effect on NB cell lines^[1].
NSC697923 (3 μM; 2 hours) can also induce apoptosis in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway^[1].
NSC697923 induces apoptosis in p53 wild-type NB cell lines by promoting p53 nuclear translocation and activation^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	Three MYCN-amplified cell lines: IMR32, NGP, NB19 and three MYCN-non-amplified cell lines: CHLA-255, SK-N-AS, and SH-SY5Y
Concentration:	0-5 μM
Incubation Time:	24 hours
Result:	Significantly reduced NB cells viability in a dose-dependent manner. Also induced cell death in the p53 non-functional cell line SK-N-AS and p53 partially functional cell line NB-19.

Western Blot Analysis^[1]

Cell Line:	p53 wild-type SH-SY5Y and IMR32 cells
Concentration:	3 μM
Incubation Time:	2 hours
Result:	Induced expression of p53-targeted gene p21 as well as the cleavage of caspase 3 in two p53 wild-type cell lines SH-SY5Y and IMR32.

体内研究
(In Vivo)

NSC697923 (5 mg/kg; i.p.; daily for 10 days) suppresses NB tumor growth in SH-SY5Y and NGP xenografts^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	5- to 6-week-old female athymic Ncr nude mice (orthotopic mouse model of NB; SH-SY5Y and NGP xenografts)^[1]
Dosage:	5 mg/kg
Administration:	I.p.; daily for 10 days
Result:	Significant tumor regression in both SH-SY5Y and NGP xenografts.

分子量

267.26

Formula

C₁₁H₉NO₅S

CAS 号

343351-67-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (374.17 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7417 mL	18.7084 mL	37.4167 mL
5 mM	0.7483 mL	3.7417 mL	7.4833 mL
10 mM	0.3742 mL	1.8708 mL	3.7417 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.35 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Cheng J, et al. A small-molecule inhibitor of UBE2N induces neuroblastoma cell death via activation of p53 and JNK pathways. Cell Death Dis. 2014;5(2):e1079. Published 2014 Feb 20.

[2]. Hodge CD, et al. Covalent Inhibition of Ubc13 Affects Ubiquitin Signaling and Reveals Active Site Elements Important for Targeting. ACS Chem Biol. 2015;10(7):1718-1728.

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Bruceantin(Synonyms: 鸦胆亭; (-)-Bruceantin; NCI165563; NSC165563)

发表于2024年3月19日由上海金畔生物科技有限公司

Bruceantin (Synonyms: 鸦胆亭; (-)-Bruceantin; NCI165563; NSC165563) 纯度: 99.06%

Bruceantin(NSC165563)可从痢鸦胆子中提取，对B16黑色素瘤，结肠癌38，L1210和白血病P388有抑制性。

Bruceantin Chemical Structure

CAS No. : 41451-75-6

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4224	In-stock
1 mg	￥1400	In-stock
5 mg	￥3500	In-stock
10 mg	￥5000	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

Bruceantin 相关产品

•相关化合物库:

Natural Product Library Plus
Bioactive Compound Library Plus
Natural Product Library
Anti-Cancer Compound Library
Traditional Chinese Medicine Monomer Library
Anti-Blood Cancer Compound Library

生物活性

Bruceantin(NSC165563) is first isolated from Brucea antidysenterica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice. IC50 value: Target: anticancer Cell differentiation was induced and c-MYC was down-regulated, suggesting a mechanistic correlation between c-MYC down-regulation and induction of cell differentiation or cell death. Treatment of HL-60 and RPMI 8226 cell lines induced apoptosis, and this involved the caspase and mitochondrial pathways. Moreover, an in vivo study using RPMI 8226 human-SCID xenografts demonstrated that bruceantin induced regression in early as well as advanced tumors, and these significant antitumor responses were facilitated in the absence of overt toxicity.

分子量

548.58

Formula

C₂₈H₃₆O₁₁

CAS 号

41451-75-6

中文名称

鸦胆亭；鸦胆停；鸦胆丁

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (182.29 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8229 mL	9.1144 mL	18.2289 mL
5 mM	0.3646 mL	1.8229 mL	3.6458 mL
10 mM	0.1823 mL	0.9114 mL	1.8229 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.56 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.56 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Cuendet M, et al. Multiple myeloma regression mediated by bruceantin. Clin Cancer Res. 2004 Feb 1;10(3):1170-9.

[2]. Cuendet M, et al. Antitumor activity of bruceantin: an old drug with new promise. J Nat Prod. 2004 Feb;67(2):269-72.

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OUL35(Synonyms: NSC39047)

发表于2024年3月15日由上海金畔生物科技有限公司

OUL35 (Synonyms: NSC39047) 纯度: 99.24%

OUL35 (NSC39047) 是选择性的 ARTD10 (PARP-10) 抑制剂，其 IC₅₀ 值为 329 nM。

OUL35 Chemical Structure

CAS No. : 6336-34-1

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥600	In-stock
5 mg	￥600	In-stock
10 mg	￥1000	In-stock
25 mg	￥2000	In-stock
50 mg	￥3200	In-stock
100 mg	￥5000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

OUL35 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Epigenetics Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Anti-Breast Cancer Compound Library
Anti-Pancreatic Cancer Compound Library

生物活性

OUL35 (NSC39047) is a potent and selective inhibitor of ARTD10 (PARP-10), with an IC₅₀ of 329 nM^[1].

IC₅₀ & Target^[1]

ARTD10/PARP10

329 nM (IC₅₀)

体外研究
(In Vitro)

OUL35 rescues HeLa cells from ARTD10-induced cell death and sensitizes cells to DNA damage. OUL35 (3 μM) binds to endogenous ARTD10 in U2OS cells^[1].
OUL35 also inhibits ARTD8 (23.4 μM), ARTD4 (22.6 μM), and ARTD15 (4.17 μM) but with modest potency^[1].
OUL35 makes hydrogen bonds to the amide and carbonyl of Gly888 and to the side-chain hydroxyl of Ser927. OUL35 stacks between Tyr919 and Tyr932, like 3AB in the crystal structure^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

256.26

Formula

C₁₄H₁₂N₂O₃

CAS 号

6336-34-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (325.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.9023 mL	19.5114 mL	39.0229 mL
5 mM	0.7805 mL	3.9023 mL	7.8046 mL
10 mM	0.3902 mL	1.9511 mL	3.9023 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (8.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (8.12 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (8.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (8.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Harikanth Venkannagari, et al. Small-Molecule Chemical Probe Rescues Cells from Mono-ADP-Ribosyltransferase ARTD10/PARP10-Induced Apoptosis and Sensitizes Cancer Cells to DNA Damage. Cell Chem Biol. 2016 Oct 20;23(10):1251-1260.

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NSC 42834(Synonyms: JAK2 Inhibitor V; Z3)

发表于2024年3月15日由上海金畔生物科技有限公司

NSC 42834 (Synonyms: JAK2 Inhibitor V; Z3) 纯度: 96.79%

NSC 42834 (JAK2 Inhibitor V) 是新型 Jak2 特异性抑制剂，能以剂量依赖的形式抑制 Jak2-V617F 和 Jak2-WT 的自磷酸化。

NSC 42834 Chemical Structure

CAS No. : 195371-52-9

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥660	In-stock
5 mg	￥600	In-stock
10 mg	￥900	In-stock
50 mg	￥3500	In-stock
100 mg	￥6500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

NSC 42834 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Immunology/Inflammation Compound Library
JAK/STAT Compound Library
Kinase Inhibitor Library
Stem Cell Signaling Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Differentiation Inducing Compound Library
Reprogramming Compound Library
Anti-Breast Cancer Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Anti-Liver Cancer Compound Library

生物活性

NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.

IC₅₀ & Target

JAK2-WT

15 μM (IC₅₀)

JAK2-V617F

28 μM (IC₅₀)

体外研究
(In Vitro)

NSC 42834 (JAK2 Inhibitor V) selectively inhibited Jak2 kinase function with no effect on Tyk2 or c-Src kinase function. NSC 42834 significantly inhibited proliferation of the Jak2-V617F-expressing, human erythroleukemia cell line, HEL 92.1.7. The NSC 42834-mediated reduction in cell proliferation correlated with reduced Jak2 and STAT3 tyrosine phosphorylation levels as well as marked cell cycle arrest. Finally, NSC 42834 inhibited the growth of hematopoietic progenitor cells isolated from the bone marrow of an essential thrombocythemia patient harboring the Jak2-V617F mutation and a polycythemia vera patient carrying a Jak2-F537I mutation.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

344.45

Formula

C₂₃H₂₄N₂O

CAS 号

195371-52-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (290.32 mM)

Ethanol : 100 mg/mL (290.32 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9032 mL	14.5159 mL	29.0318 mL
5 mM	0.5806 mL	2.9032 mL	5.8064 mL
10 mM	0.2903 mL	1.4516 mL	2.9032 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.26 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.26 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (7.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Jacqueline Sayyah, Andrew Magis, David A. Ostrov, et al. Z3, a novel Jak2 tyrosine kinase small-molecule inhibitor that suppresses Jak2-mediated pathologic cell growth . Mol Cancer Ther 2008;7(8):2308-18.

[2]. Jacqueline Sayyah, Peter P. Sayeski. Jak2 inhibitors: Rationale and role as therapeutic agents in hematologic malignancies. Current Oncology Reports. 2009, 11(2): 117-124.

[3]. Ehab Atallah , Srdan Verstovsek . Prospect of JAK2 inhibitor therapy in myeloproliferative neoplasms. Expert Review of Anticancer Therapy. 2009,9 (5):663-670.

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Veratramine(Synonyms: 黎芦碱; NSC17821; NSC23880)

发表于2024年3月15日由上海金畔生物科技有限公司

Veratramine (Synonyms: 黎芦碱; NSC17821; NSC23880) 纯度: 99.61%

Veratramine(NSC17821; NSC23880)是信号转导抑制剂，可作用于肿瘤。

Veratramine Chemical Structure

CAS No. : 60-70-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥550	In-stock
5 mg	￥500	In-stock
10 mg	￥800	In-stock
50 mg	￥3200	In-stock
100 mg	￥5100	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Veratramine 相关产品

•相关化合物库:

Natural Product Library Plus
Bioactive Compound Library Plus
Natural Product Library
Anti-Cancer Compound Library
Alkaloids Library

生物活性

Veratramine(NSC17821; NSC23880) is useful as a signal transduction inhibitor for treating tumors.

分子量

409.60

Formula

C₂₇H₃₉NO₂

CAS 号

60-70-8

中文名称

黎芦碱；黎芦胺；藜芦铵

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (244.14 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4414 mL	12.2070 mL	24.4141 mL
5 mM	0.4883 mL	2.4414 mL	4.8828 mL
10 mM	0.2441 mL	1.2207 mL	2.4414 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.10 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.10 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.10 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Wang L, et al. Hypotensive effect and toxicology of total alkaloids and veratramine from roots and rhizomes of Veratrum nigrum L. in spontaneously hypertensive rats. Pharmazie. 2008 Aug;63(8):606-10.

[2]. Li HJ, et al. Puqienine F, a novel veratramine alkaloid from the bulbs of Fritillaria puqiensis. Chem Pharm Bull (Tokyo). 2006 May;54(5):722-4.

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Mivobulin(Synonyms: NSC 613862; (S)-(-)-NSC 613862)

发表于2024年3月13日由上海金畔生物科技有限公司

Mivobulin (Synonyms: NSC 613862; (S)-(-)-NSC 613862)

Mivobulin (NSC 613862) 是一种微管蛋白 (tubulin) 抑制剂，在与秋水仙碱重叠的区域结合微管蛋白，抑制其聚合。Mivobulin (NSC 613862) 在微管蛋白二聚体中可促进异常聚合物的形成和 GTPase 的活性。具有抗肿瘤活性。

Mivobulin Chemical Structure

CAS No. : 122332-18-7

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性	Mivobulin (NSC 613862) is a tubulin inhibitor, binds to tubulin in the region that overlaps the colchicine site, and inhibits tubulin polymerization. Mivobulin (NSC 613862) promotes the formation of abnormal polymers and a GTPase activity in the tubulin dimer. Anti-cancer activity^[1].
IC₅₀ & Target	Tubulin^[1]
分子量	325.37
Formula	C₁₇H₁₉N₅O₂
CAS 号	122332-18-7
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Barbier P, et al. The active GTP- and ground GDP-liganded states of tubulin are distinguished by the binding of chiral isomers of ethyl 5-amino-2-methyl-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-yl carbamate. Biochemistry. 1998 Jan 13;37(2):758-68.

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BPH-1358(Synonyms: NSC50460)

发表于2024年3月13日由上海金畔生物科技有限公司

BPH-1358 (Synonyms: NSC50460)

BPH-1358 (NSC50460) 是一种有效的人 FPPS 和 UPPS 抑制剂，IC₅₀ 值分别为 1.8 μM 和 110 nM，在体外对金黄色葡萄球菌的 MIC 值大约为 250 ng/mL。

BPH-1358 Chemical Structure

CAS No. : 5352-53-4

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

生物活性

BPH-1358 (NSC50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC₅₀s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL)^[1]^[2].

IC₅₀ & Target

IC50: 1.8 μM (human bisphosphonate farnesyl diphosphate synthase)^[1]; 100 nM (undecaprenyl diphosphate synthase)^[2]

体外研究
(In Vitro)

BPH-1358 is the most potent inhibitor of both E. coli UPPS (EcUPPS) as well as S. aureus UPPS (SaUPPS) with an IC₅₀ of 110 nM. BPH-1358 against E. coli and S. aureus with EC₅₀ of 300 nM and 290 nM, respectively^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

BPH-1358 is active against S. aureus in vivo (20/20 mice survived in an i.p. infection model with a MRSA strain)^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

601.53

Formula

C₃₂H₃₀Cl₂N₆O₂

CAS 号

5352-53-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

In Vitro:

DMSO : 6.25 mg/mL (10.39 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6624 mL	8.3121 mL	16.6243 mL
5 mM	0.3325 mL	1.6624 mL	3.3249 mL
10 mM	0.1662 mL	0.8312 mL	1.6624 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 0.62 mg/mL (1.03 mM); Clear solution

此方案可获得 ≥ 0.62 mg/mL (1.03 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 6.2 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 0.62 mg/mL (1.03 mM); Clear solution

此方案可获得 ≥ 0.62 mg/mL (1.03 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 6.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。

参考文献

[1]. Zhu W, et al. Antibacterial drug leads: DNA and enzyme multitargeting. J Med Chem. 2015 Feb 12;58(3):1215-27.

[2]. Liu YL, et al. Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries. ACS Med Chem Lett. 2015 Jan 29;6(3):349-54.

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(E/Z)-BCI(Synonyms: NSC 150117)

发表于2024年3月11日由上海金畔生物科技有限公司

(E/Z)-BCI (Synonyms: NSC 150117)

(E/Z)-BCI (NSC 150117) 是一种 DUSP6 抑制剂，具有抗炎活性。(E/Z)-BCI 通过激活 Nrf2 信号和抑制 NF-κB 通路，减弱 LPS 诱导的巨噬细胞炎症和 ROS 生成。

(E/Z)-BCI Chemical Structure

CAS No. : 15982-84-0

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生物活性

(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway^[1].

IC₅₀ & Target

DUSP6^[1]

体外研究
(In Vitro)

(E/Z)-BCI hydrochloride (2-10 μM; 72 hours) significantly decreases cell viability in a time and dose-dependent manner in gastric epithelial cell GES1, GC cell lines, and AGS cell lines^[2].
(E/Z)-BCI hydrochloride (0.5-4 μM; 24 hours) significantly inhibits DUSP6 expression in LPS-activated macrophages^[1].
(E/Z)-BCI hydrochloride (0.5-2 μM; 24 hours) treatment significantly inhibits the expression of IL-1β, TNF-α and IL-6 mRNA in LPS-activated macrophages^[1].
(E/Z)-BCI hydrochloride decreases ROS production and activates the Nrf2 pathway in LPS-activated macrophages^[1]. (E/Z)-BCI hydrochloride inhibits cell proliferation, migration and invasion in a receptor-independent manner and enhances Cisplatin (CDDP) cytotoxicity (enhances CDDP-induced cell death and apoptosis) at pharmacological concentrations in the gastric cancer (GC) cells^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:	Gastric epithelial cell GES1, GC cell lines (HGC27, SGC7901, MKN45, BGC823, MGC803, SNU216, NUGC4), AGS cell lines
Concentration:	2 μM, 4 μM, 6 μM, 8 μM, 10 μM
Incubation Time:	72 hours
Result:	Cell viability was significantly decreased in a time and dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:	RAW264.7 macrophage cells (by LPS-activated macrophages)
Concentration:	0.5 μM, 1 μM, 2 μM, 4 μM
Incubation Time:	24 hours
Result:	DUSP6 protein was significantly downregulated in LPS-activated macrophages.

RT-PCR^[1]

Cell Line:	RAW264.7 macrophage cells (by LPS-activated macrophages)
Concentration:	0.5 μM, 1 μM, 2 μM
Incubation Time:	24 hours
Result:	The expression of IL-1β, TNF-α and IL-6 mRNA was significantly inhibited in LPS-activated macrophages.

体内研究
(In Vivo)

(E/Z)-BCI hydrochloride (35 mg/kg; intraperitoneal injection; every 7 days; for four weeks; female BALB/c nude mice) treatment enhances cisplatin efficacy in PDX models^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Patient-derived xenograft (PDX) models (4-5-week-old female BALB/c nude mice)^[2]
Dosage:	35 mg/kg
Administration:	Intraperitoneal injection; every 7 days; for four weeks
Result:	Tumor weights in the PDX models treated plus CDDP were significantly suppressed compared with tumors from PDX model mice treated with either agent alone.

分子量

317.42

Formula

C₂₂H₂₃NO

CAS 号

15982-84-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Zhang F, et al. DUSP6 Inhibitor (E/Z)-BCI Hydrochloride Attenuates Lipopolysaccharide-Induced Inflammatory Responses in Murine Macrophage Cells via Activating the Nrf2 Signaling Axis and Inhibiting the NF-κB Pathway. Inflammation. 2019 Apr;42(2):672-681.

[2]. Wu QN,et al. Pharmacological inhibition of DUSP6 suppresses gastric cancer growth and metastasis and overcomes cisplatin resistance. Cancer Lett. 2018 Jan 1;412:243-255.

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