标签归档：ski

RU-SKI 43 hydrochloride(Synonyms: RU-SKI 43（盐酸盐）)

发表于由

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。

RU-SKI 43 hydrochloride (Synonyms: RU-SKI 43（盐酸盐）) 纯度: 98.54%

RU-SKI 43 hydrochloride 是一种有效的选择性刺猬酰基转移酶 (Hhat) 抑制剂，IC50 为 850 nM。RU-SKI 43 hydrochloride 通过独立于平滑化的非规范信号传导降低 Gli-1 激活，并抑制 Akt 和 mTOR 通路活性。RU-SKI 43 hydrochloride 具有抗癌活性。

RU-SKI 43 hydrochloride(Synonyms: RU-SKI 43（盐酸盐）)

RU-SKI 43 hydrochloride Chemical Structure

CAS No. : 1782573-67-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1024 In-stock
2 mg ￥800 In-stock
5 mg ￥1100 In-stock
10 mg ￥1600 In-stock
50 mg ￥6900 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

RU-SKI 43 hydrochloride 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
  • Differentiation Inducing Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

RU-SKI 43 hydrochloride is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 hydrochloride reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 hydrochloride has anti-cancer activity[1].

IC50 & Target

IC50: 850 nM (Hhat)[1]
体外研究
(In Vitro)

RU-SKI 43 hydrochloride (10 μM; for 6 days) strongly decreases cell proliferation (83% in AsPC-1 cells) in AsPC-1 and Panc-1 cells[2].
RU-SKI 43 hydrochloride (10 or 20 μM; 5 hours) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours[1].
RU-SKI 43 hydrochloride (10 μM; for 72 hours) causes a 40% decrease in Gli-1 levels in AsPC-1 cells[2].
RU-SKI 43 hydrochloride (10 μM; 48 hours) results in decreased phosphorylation (47-67%) of four proteins in the Akt pathway, including Akt (phosphorylation at both Thr307 and Ser473), PRAS40, Bad and GSK-3β. RU-SKI 43 treatment also decreases phosphorylation of mTOR and S6, members of the mTOR signaling pathway[2].
RU-SKI 43 hydrochloride behaves as an uncompetitive inhibitor (Ki=7.4 μM) with respect to Shh, and as a noncompetitive inhibitor (Ki=6.9 μM) with respect to 125I-iodo-palmitoylCoA[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 Proliferation Assay[2]

Cell Line: AsPC-1 and Panc-1 pancreatic cancer cells
Concentration: 10 μM
Incubation Time: For 6 days (drugs were replenished every 48 hours)
Result: Strongly decreased cell proliferation (83% in AsPC-1 cells).

Western Blot Analysis[1]

Cell Line: COS-1 cells expressing HA-Hhat and Shh
Concentration: 10 or 20 μM
Incubation Time: 5 hours
Result: Caused dose-dependent inhibition of Shh palmitoylation following only 5 hours.

体内研究
(In Vivo)

RU-SKI 43 hydrochloride has a t1/2 of 17 min in mouse plasma after IV administration[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

423.01

Formula

C22H31ClN2O2S
CAS 号

1782573-67-4
中文名称

RU-SKI 43（盐酸盐）
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : ≥ 51 mg/mL (120.56 mM)

H2O : 2.5 mg/mL (5.91 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 2.3640 mL 11.8201 mL 23.6401 mL
5 mM 0.4728 mL 2.3640 mL 4.7280 mL
10 mM 0.2364 mL 1.1820 mL 2.3640 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 (sealed storage, away from moisture)。-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: ≥ 2.5 mg/mL (5.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.91 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 (5.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.91 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
*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]. Petrova E, et al. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling.Nat Chem Biol. 2013 Apr;9(4):247-9.

    [2]. Petrova E, et al. Hedgehog acyltransferase as a target in pancreatic ductal adenocarcinoma. Oncogene. 2014 Jan 27. doi: 10.1038/onc.2013.575.

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

SKI-178

发表于由

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。

SKI-178  纯度: 98.05%

SKI-178 是一种有效的鞘氨醇激酶-1 (SphK1) 和 SphK2 抑制剂。SKI-178 对药物敏感和多药耐药癌细胞系 (如MTR3、NCI-ADR 和 HL60/VCR) 的 IC50 浓度范围为 1.8 到 0.1 μM。SKI-178 以 CDK1 依赖性方式诱导人急性髓性白血病细胞凋亡。

SKI-178

SKI-178 Chemical Structure

CAS No. : 1259484-97-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥830 In-stock
5 mg ￥750 In-stock
10 mg ￥1300 In-stock
25 mg ￥2500 In-stock
50 mg ￥4000 In-stock
100 mg ￥6000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SKI-178 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines[1][2].

体外研究
(In Vitro)

SKI-178 (5 μM; 24 hours)-induced apoptotic cell death correlates with prolonged Bcl-2 phosphorylation[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.

Apoptosis Analysis[1]

Cell Line: HL-60 cells
Concentration: 5 μM
Incubation Time: 24 hours
Result: JNK activity (indicated by phosphorylation at Thr183/Tyr185) increased in a time-dependent manner starting as early as 2 hours continued to increase for at least 24 hours. There was a concomitant increase in apoptotic cell death indicated by the cleavage of caspase-7. Bcl-2 phosphorylation at Ser70 increased with time in response to SKI-178 treatment, reaching maximal levels at 8 hours, which was consistent with the timing of caspase-7 activation.

体内研究
(In Vivo)

SKI-178 (20 mg/kg; retro-orbital injection under isoflurane anesthesia) inhibits leukemic progression in the MLL-AF9 model[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.

Animal Model: MLL-AF9 mouse model (leukemic mice)[3]
Dosage: 20 mg/kg
Administration: Retro-orbital injection under isoflurane anesthesia; three times per week for 1 and 3 weeks
Result: White blood cell (WBC) counts decreased from their initial 104 cells/μL levels and continued to decline after 3 weeks of treatment until they reached normal levels (~4×103 cells/μL).

分子量

394.42

Formula

C21H22N4O4
CAS 号

1259484-97-3
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 : 50 mg/mL (126.77 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5354 mL 12.6768 mL 25.3537 mL
5 mM 0.5071 mL 2.5354 mL 5.0707 mL
10 mM 0.2535 mL 1.2677 mL 2.5354 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：

——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: 2.5 mg/mL (6.34 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.34 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% corn oil

    Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.34 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]. Hengst JA, et al. SKI-178: A Multitargeted Inhibitor of Sphingosine Kinase and Microtubule Dynamics Demonstrating Therapeutic Efficacy in Acute Myeloid Leukemia Models. Cancer Transl Med. 2017;3(4):109-121.

    [2]. Hengst JA, et al. Development of a sphingosine kinase 1 specific small-molecule inhibitor. Bioorg Med Chem Lett. 2010;20(24):7498-7502.

    [3]. Dick TE, et al. The apoptotic mechanism of action of the sphingosine kinase 1 selective inhibitor SKI-178 in human acute myeloid leukemia cell lines. J Pharmacol Exp Ther. 2015;352(3):494-508.

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

SKI V

发表于由

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。

SKI V  纯度: 98.09%

SKI V 是一种非竞争性的，有效的非脂质鞘氨醇激酶 (SPHK; SK) 抑制剂，对 GST-hSK 的 IC50 为 2 μM。 SKI V 有效抑制 PI3K，对 hPI3k 的 IC50 为 6 μM。SKI V 减少有丝分裂的第二信使鞘氨醇-1-磷酸 (S1P) 的形成。SKI V 诱导细胞凋亡 (apoptosis) 并具有抗肿瘤活性。

SKI V

SKI V Chemical Structure

CAS No. : 24418-86-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3080 In-stock
5 mg ￥2800 In-stock
10 mg ￥4500 In-stock
50 mg ￥12500 In-stock
100 mg 询价

* Please select Quantity before adding items.

SKI V 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC50 of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity[1][2].

IC50 & Target

IC50: 2 μM (GST-hSK), 6 μM (hPI3k) and 80 μM (ERK2)[1]
体外研究
(In Vitro)

SKI V has weak activity toward ERK2 (IC50 of 80 μM for hERK2) and does not inhibit PKC-α[1].
SKI V (10 μM; for 24 hours) inhibits cancer cell proliferation and induces apoptosis[1].
SKI V (0.2, 1, 5 μM; pretreated for 1 hour) decreases phospho-Akt and phospho-MEK levels. Near-confluent cultures of JC cells are serum-starved for 16 hours, followed by pretreatment SKI V for 1 hour[2].
SKI V has IC50s for inhibition of sphingosine kinase (SK) and tumor cell proliferation of ∼2 μM[1].
SKI V (20 μg/ml) inhibits not only purified but endogenous SK in in MDA-MB-231 cells[1].
SKI V (0.2, 1, 5 μM) inhibits intracellular S1P formation in JC cells in a dose-dependent fashion[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.

Cell Proliferation Assay[1]

Cell Line: T24 tumor cells
Concentration: 10 μM
Incubation Time: For 24 hours
Result: Inhibited cancer cell proliferation.

Apoptosis Analysis[1]

Cell Line: T24 tumor cells
Concentration: 10 μM
Incubation Time: For 24 hours
Result: Induced apoptosis.

Western Blot Analysis[2]

Cell Line: JC cells
Concentration: 0.2, 1, 5 μM
Incubation Time: Pretreated for 1 hour
Result: Decreased phospho-Akt and phospho-MEK levels.

体内研究
(In Vivo)

SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly lowers tumor growth (>50% decreased at day 18) than control animals[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: 6-8 weeks old BALB/c female mice with JC mammary adenocarcinoma cells[1]
Dosage: 75 mg/kg
Administration: IP; days 1, 5, 9, 15
Result: Tumor growth was significantly lower (>50% decreased at day 18) than tumor growth in control animals.

分子量

254.24

Formula

C15H10O4
CAS 号

24418-86-8
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 : 250 mg/mL (983.32 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9333 mL 19.6665 mL 39.3329 mL
5 mM 0.7867 mL 3.9333 mL 7.8666 mL
10 mM 0.3933 mL 1.9666 mL 3.9333 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：

——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 (8.18 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.18 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 (8.18 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.18 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
*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]. French KJ, et al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.

    [2]. French KJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603.

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

RU-SKI 43

发表于由

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。

RU-SKI 43 

RU-SKI 43 是一种有效的选择性刺猬酰基转移酶 (Hhat) 抑制剂，IC50 为 850 nM。RU-SKI 43 通过独立于平滑化的非规范信号传导降低 Gli-1 激活，并抑制 Akt 和 mTOR 通路活性。RU-SKI 43 具有抗癌活性。

RU-SKI 43

RU-SKI 43 Chemical Structure

CAS No. : 1043797-53-0

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

* Please select Quantity before adding items.

RU-SKI 43 的其他形式现货产品:

RU-SKI 43 hydrochloride

生物活性

RU-SKI 43 is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 has anti-cancer activity[1].

IC50 & Target

IC50: 850 nM (Hhat)[1]
体外研究
(In Vitro)

RU-SKI 43 (10 μM; for 6 days) strongly decreases cell proliferation (83% in AsPC-1 cells) in AsPC-1 and Panc-1 cells[2].
RU-SKI 43 (10 or 20 μM; 5 hours) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours[1].
RU-SKI 43 (10 μM; for 72 hours) causes a 40% decrease in Gli-1 levels in AsPC-1 cells[2].
RU-SKI 43 (10μM; 48 hours) results in decreased phosphorylation (47-67%) of four proteins in the Akt pathway, including Akt (phosphorylation at both Thr307 and Ser473), PRAS40, Bad and GSK-3β. RU-SKI 43 treatment also decreases phosphorylation of mTOR and S6, members of the mTOR signaling pathway[2].
RU-SKI 43 behaves as an uncompetitive inhibitor (Ki=7.4 μM) with respect to Shh, and as a noncompetitive inhibitor (Ki=6.9 μM) with respect to 125I-iodo-palmitoylCoA[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 Proliferation Assay[2]

Cell Line: AsPC-1 and Panc-1 pancreatic cancer cells
Concentration: 10 μM
Incubation Time: For 6 days (drugs were replenished every 48 hours)
Result: Strongly decreased cell proliferation (83% in AsPC-1 cells).

Western Blot Analysis[1]

Cell Line: COS-1 cells expressing HA-Hhat and Shh
Concentration: 10 or 20 μM
Incubation Time: 5 hours
Result: Caused dose-dependent inhibition of Shh palmitoylation following only 5 hours.

体内研究
(In Vivo)

RU-SKI 43 has a t1/2 of 17 min in mouse plasma after IV administration[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

386.55

Formula

C22H30N2O2S
CAS 号

1043797-53-0
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]. Petrova E, et al. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling.Nat Chem Biol. 2013 Apr;9(4):247-9.

    [2]. Petrova E, et al. Hedgehog acyltransferase as a target in pancreatic ductal adenocarcinoma. Oncogene. 2014 Jan 27. doi: 10.1038/onc.2013.575.

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SKI-I

发表于由

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。

SKI-I 

SKI-I 是一种有效和选择性的人鞘氨醇激酶 (SK) 抑制剂，抑制 ST-hSK 的 IC50 值为 1.2 μM。SKI-I 还抑制 hERK2 (IC50=11 μM)。SKI-I 在肿瘤细胞系中诱导细胞凋亡。

SKI-I

SKI-I Chemical Structure

CAS No. : 306301-68-8

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生物活性

SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines[1][2].

IC50 & Target

IC50: 1.2 μM (ST-hSK); 11 μM (hERK2)[1]
体外研究
(In Vitro)

SKI-I (Compound I; 5 μg/mL) inhibits SK activity by 99%[1].
SKI-I (10 μM; 24 h) induces the apoptosis of T24 cells[1].

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

406.44

Formula

C25H18N4O2
CAS 号

306301-68-8
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]. French KJ, et, al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.

    [2]. Sharma AK, et, al. Synthesis and bioactivity of sphingosine kinase inhibitors and their novel aspirinyl conjugated analogs. Eur J Med Chem. 2010 Sep;45(9):4149-56.

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SKI-I

发表于由

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。

SKI-I 

SKI-I 是一种有效和选择性的人鞘氨醇激酶 (SK) 抑制剂，抑制 ST-hSK 的 IC50 值为 1.2 μM。SKI-I 还抑制 hERK2 (IC50=11 μM)。SKI-I 在肿瘤细胞系中诱导细胞凋亡。

SKI-I

SKI-I Chemical Structure

CAS No. : 306301-68-8

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500 mg   询价  

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生物活性

SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines[1][2].

IC50 & Target

IC50: 1.2 μM (ST-hSK); 11 μM (hERK2)[1]
体外研究
(In Vitro)

SKI-I (Compound I; 5 μg/mL) inhibits SK activity by 99%[1].
SKI-I (10 μM; 24 h) induces the apoptosis of T24 cells[1].

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

406.44

Formula

C25H18N4O2
CAS 号

306301-68-8
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]. French KJ, et, al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.

    [2]. Sharma AK, et, al. Synthesis and bioactivity of sphingosine kinase inhibitors and their novel aspirinyl conjugated analogs. Eur J Med Chem. 2010 Sep;45(9):4149-56.

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

SKI-I

发表于由

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。

SKI-I 

SKI-I 是一种有效和选择性的人鞘氨醇激酶 (SK) 抑制剂，抑制 ST-hSK 的 IC50 值为 1.2 μM。SKI-I 还抑制 hERK2 (IC50=11 μM)。SKI-I 在肿瘤细胞系中诱导细胞凋亡。

SKI-I

SKI-I Chemical Structure

CAS No. : 306301-68-8

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

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生物活性

SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines[1][2].

IC50 & Target

IC50: 1.2 μM (ST-hSK); 11 μM (hERK2)[1]
体外研究
(In Vitro)

SKI-I (Compound I; 5 μg/mL) inhibits SK activity by 99%[1].
SKI-I (10 μM; 24 h) induces the apoptosis of T24 cells[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

406.44

Formula

C25H18N4O2
CAS 号

306301-68-8
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]. French KJ, et, al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.

    [2]. Sharma AK, et, al. Synthesis and bioactivity of sphingosine kinase inhibitors and their novel aspirinyl conjugated analogs. Eur J Med Chem. 2010 Sep;45(9):4149-56.

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

CAY10621(Synonyms: SKI 5C)

发表于由

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。

CAY10621 (Synonyms: SKI 5C)

CAY10621 (SKI 5C; Compound 5c) 是一种特异性的鞘氨醇激酶 1 (SPHK1) 抑制剂，IC50 为 3.3 μM。CAY10621 对细胞具有低毒性。CAY10621 具有抗癌肿瘤研究的潜力。

CAY10621(Synonyms: SKI 5C)

CAY10621 Chemical Structure

CAS No. : 120005-55-2

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生物活性

CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research[1].

分子量

435.64

Formula

C26H45NO4
CAS 号

120005-55-2
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]. Lingkai Wong, et al. Synthesis and evaluation of sphingosine analogues as inhibitors of sphingosine kinases. J Med Chem. 2009 Jun 25;52(12):3618-26.

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CAY10621(Synonyms: SKI 5C)

发表于由

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。

CAY10621 (Synonyms: SKI 5C)

CAY10621 (SKI 5C; Compound 5c) 是一种特异性的鞘氨醇激酶 1 (SPHK1) 抑制剂，IC50 为 3.3 μM。CAY10621 对细胞具有低毒性。CAY10621 具有抗癌肿瘤研究的潜力。

CAY10621(Synonyms: SKI 5C)

CAY10621 Chemical Structure

CAS No. : 120005-55-2

规格 是否有货
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250 mg   询价  
500 mg   询价  

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生物活性

CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research[1].

分子量

435.64

Formula

C26H45NO4
CAS 号

120005-55-2
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]. Lingkai Wong, et al. Synthesis and evaluation of sphingosine analogues as inhibitors of sphingosine kinases. J Med Chem. 2009 Jun 25;52(12):3618-26.

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

CAY10621(Synonyms: SKI 5C)

发表于由

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。

CAY10621 (Synonyms: SKI 5C)

CAY10621 (SKI 5C; Compound 5c) 是一种特异性的鞘氨醇激酶 1 (SPHK1) 抑制剂，IC50 为 3.3 μM。CAY10621 对细胞具有低毒性。CAY10621 具有抗癌肿瘤研究的潜力。

CAY10621(Synonyms: SKI 5C)

CAY10621 Chemical Structure

CAS No. : 120005-55-2

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

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生物活性

CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research[1].

分子量

435.64

Formula

C26H45NO4
CAS 号

120005-55-2
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]. Lingkai Wong, et al. Synthesis and evaluation of sphingosine analogues as inhibitors of sphingosine kinases. J Med Chem. 2009 Jun 25;52(12):3618-26.

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

Heptaplatin(Synonyms: SKI 2053R)

发表于由

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。

Heptaplatin (Synonyms: SKI 2053R)

Heptaplatin (SKI 2053R) 是一种铂衍生物，对多种癌细胞系具有抗癌活性，包括对顺铂耐药的肿瘤细胞系。SKI-2053R 在胃腺癌的研究中具有活性，具有良好的毒性特征。

Heptaplatin(Synonyms: SKI 2053R)

Heptaplatin Chemical Structure

CAS No. : 146665-77-2

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生物活性

Heptaplatin (SKI 2053R) is a platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant tumor cell lines. SKI-2053R is active in the research of gastric adenocarcinoma and has favorable toxicity profiles[1].

分子量

471.36

Formula

C11H20N2O6Pt
CAS 号

146665-77-2
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]. Kim NK, et al. Phase II clinical trial of SKI-2053R, a new platinum analog, in the treatment of patients with advanced gastric adenocarcinoma. Cancer. 1999;86(7):1109-1115.

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Bosutinib D8(Synonyms: SKI-606 D8)

发表于由

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。

Bosutinib D8 (Synonyms: SKI-606 D8)

Bosutinib D8 (SKI-606 D8) 是 Bosutinib 的氘代物。Bosutinib 是 Src/Abl 的双抑制剂， IC50 分别为 1.2 nM 和 1 nM。

Bosutinib D8(Synonyms: SKI-606 D8)

Bosutinib D8 Chemical Structure

规格 价格 是否有货
1 mg ￥2250 询问价格 & 货期

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生物活性

Bosutinib D8 (SKI-606 D8) is a deuterium labeled Bosutinib. Bosutinib is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively[1][2].

IC50 & Target

IC50: 1.2 nM (Src), 1 nM (Abl)[1]
分子量

538.50

Formula

C26H21D8Cl2N5O3
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
参考文献

  • [1]. Boschelli DH, et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J Med Chem, 2001, 44(23), 3965-3977.

    [2]. Golas JM, et al. SKI-606, a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiproliferative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice. Cancer Res, 2003, 63(2), 375-381.

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SKI II

发表于由

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。

SKI II  纯度: 99.88%

SKI II 是一种合成的、口服有效的鞘氨醇激酶 (SK) 抑制剂, 抑制 SK1 和 SK2, IC50值分别为 78 μM 和 45 μM。SKI II 通过诱导溶酶体和/或蛋白酶体降解导致SK1的不可逆抑制。

SKI II

SKI II Chemical Structure

CAS No. : 312636-16-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥605 In-stock
5 mg ￥550 In-stock
10 mg ￥700 In-stock
25 mg ￥1200 In-stock
50 mg ￥2100 In-stock
100 mg ￥3700 In-stock
200 mg ￥6600 In-stock
500 mg   询价  
1 g   询价  

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SKI II 相关产品

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生物活性

SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation[1][2].

IC50 & Target

IC50 value: 78/45 μM (SK1/2)[1][2].
体外研究
(In Vitro)

SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II promotes the degradation of β-catenin by enhancing Wnt5A[1].
SKI II (1.25 μM, 48 h) in combination with DDP has a clear synergistic effect in human gastric carcinoma SGC7901/DDP cell line[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.

Cell Cytotoxicity Assay[1]

Cell Line: The human gastric carcinoma SGC7901/DDP cell line.
Concentration: 0 μM, 1.25 μM (combined with DDP).
Incubation Time: 48 hours.
Result: SKI II in combination with DDP had a greater effect on the SGC-7901/DDP cells compared with DDP or SKI II alone.

体内研究
(In Vivo)

Chronic SKI II (50.0 mg/kg, 3-weekly i.p. for 16 weeks) administration leads to permanent reduction of S1P concentrations in plasma in mice[3].
SKI II (50.0 mg/kg, IP; 100 mg/kg, PO) treatment reduces tumor growth in mice bearing solid tumor model[4].

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: 8 week-old female LDL-R-/- mice[3].
Dosage: 50.0 mg/kg.
Administration: IP injection daily, 3 days a week for 16 weeks.
Result: A single administration of produced a significant reduction of plasma S1P with the maximum (~40%) observed 12 h after injection. At sacrifice (72 h after last injection) S1P levels were 266 ± 18 ng/mL and 328 ± 30 ng/mL in the SKI-II-treated and control groups, respectively.
Animal Model: BALB/c mouse solid tumor model that uses JC mammary adenocarcinoma cells[4].
Dosage: 50.0 mg/kg.
Administration: IP injection daily, 3 days a week for 16 weeks.
Result: Had strong inhibition of tumor growth from the start of treatment of 65%, with no toxicity or weight loss.
Animal Model: BALB/c JC tumor model[4].
Dosage: 100 mg/kg.
Administration: PO every other day.
Result: Caused significant antitumor activity in well-established tumors as early as day 5, with maximal response seen at the end of the study. Showed 79% inhibition of tumor growth from the start of treatment.

分子量

302.78

Formula

C15H11ClN2OS
CAS 号

312636-16-1
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 (330.27 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 3.3027 mL 16.5136 mL 33.0273 mL
5 mM 0.6605 mL 3.3027 mL 6.6055 mL
10 mM 0.3303 mL 1.6514 mL 3.3027 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：

——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: ≥ 2.75 mg/mL (9.08 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (9.08 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 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: ≥ 2.75 mg/mL (9.08 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (9.08 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 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]. Liu H, et al. SphK1 inhibitor SKI II inhibits the proliferation of human hepatoma HepG2 cells via the Wnt5A/β-catenin signaling pathway. Life Sci. 2016 Apr 15;151:23-9.

    [2]. Potì F, et al. SKI-II–a sphingosine kinase 1 inhibitor–exacerbates atherosclerosis in low-density lipoprotein receptor-deficient (LDL-R-/-) mice on high cholesterol diet. Atherosclerosis. 2015 May;240(1):212-5.

    [3]. Liu Y, et al. SKI-II reverses the chemoresistance of SGC7901/DDP gastric cancer cells. Oncol Lett. 2014 Jul;8(1):367-373.

    [4]. French KJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603.

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