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ARD-2585

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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。

ARD-2585  纯度: 99.48%

ARD-2585 是有效的、具有口服活性的雄激素受体 (androgen receptor) 的PROTAC 降解剂。

ARD-2585

ARD-2585 Chemical Structure

规格 价格 是否有货 数量
5 mg ￥9600 In-stock
10 mg ￥15500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

ARD-2585 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor[1].

体外研究
(In Vitro)

ARD-2585 achieves DC50 values of 0.04-0.1 nM in the VCaP cell line with AR gene amplification and in the LNCaP cell line carrying an AR mutation[1].
ARD-2585 (100 nM) is effective in reducing the AR protein level at the 3 and 24 h time-points by 78% (p < 0.01) and 60% at the 6 h time-point (p > 0.05)[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

763.28

Formula

C41H43ClN8O5
运输条件

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

-20°C, sealed storage, away from moisture and light

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

DMSO : 85 mg/mL (111.36 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3101 mL 6.5507 mL 13.1014 mL
5 mM 0.2620 mL 1.3101 mL 2.6203 mL
10 mM 0.1310 mL 0.6551 mL 1.3101 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 and 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: 4.25 mg/mL (5.57 mM); Suspended solution; Need ultrasonic

    此方案可获得 4.25 mg/mL (5.57 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 42.5 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: ≥ 4.25 mg/mL (5.57 mM); Clear solution

    此方案可获得 ≥ 4.25 mg/mL (5.57 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 42.5 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]. Weiguo Xiang. et al. Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer. J Med Chem. 2021 Sep 23;64(18):13487-13509.

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dBET23

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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。

dBET23  纯度: 99.33%

dBET23 是一种高效、选择性的 PROTAC BRD4 降解剂，对 BRD4BD1 蛋白的 DC50/5h 约为 50 nM。

dBET23

dBET23 Chemical Structure

CAS No. : 1957234-83-1

规格 价格 是否有货 数量
1 mg ￥3900 In-stock
5 mg ￥11500 In-stock
10 mg ￥18000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

dBET23 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

dBET23 is a highly effective and selective PROTAC BRD4 degrader with a DC50/5h of ~ 50 nM for BRD4BD1 protein[1].

体外研究
(In Vitro)

dBET23 occupies the canonical binding sites on CRBN and BRD4BD1 for thalidomide and JQ1, respectively[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

885.38

Formula

C43H45ClN8O9S
CAS 号

1957234-83-1
运输条件

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

-20°C, sealed storage, away from moisture and light

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

DMSO : 110 mg/mL (124.24 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 1.1295 mL 5.6473 mL 11.2946 mL
5 mM 0.2259 mL 1.1295 mL 2.2589 mL
10 mM 0.1129 mL 0.5647 mL 1.1295 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 and 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    90% corn oil

    Solubility: ≥ 4.25 mg/mL (4.80 mM); Suspended solution

    此方案可获得 ≥ 4.25 mg/mL (4.80 mM，饱和度未知) 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 42.5 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]. Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018;14(7):706-714.

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m-PEG36-amine

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m-PEG36-amine 

m-PEG36-amine 是一种 PROTAC linker，属于 PEG 类。可用于合成 PROTAC 分子。

m-PEG36-amine

m-PEG36-amine Chemical Structure

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

m-PEG36-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

1616.97

Formula

C3H9NO
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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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

Tos-PEG20-Tos

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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。

Tos-PEG20-Tos 

Tos-PEG20-Tos 是一种 PROTAC linker，属于 PEG 类。可用于合成 PROTAC 分子。

Tos-PEG20-Tos

Tos-PEG20-Tos Chemical Structure

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

Tos-PEG20-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

1207.44

Formula

C54H94O25S2
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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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

Tos-PEG21-Tos

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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。

Tos-PEG21-Tos 

Tos-PEG21-Tos 是一种 PROTAC linker，属于 PEG 类。可用于合成 PROTAC 分子。

Tos-PEG21-Tos

Tos-PEG21-Tos Chemical Structure

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

Tos-PEG21-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

1251.49

Formula

C56H98O26S2
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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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

THS-044

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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。

THS-044 

THS-044结合且稳定化HIF2αPAS-B折叠状态, 调节HIF2活性。

THS-044

THS-044 Chemical Structure

CAS No. : 62054-67-5

规格 价格 是否有货 数量
1 mg ￥2000 In-stock
5 mg ￥3500 In-stock
10 mg ￥5000 In-stock
50 mg ￥18000 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

THS-044 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Oxygen Sensing Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Transcription Factor Targeted Library

生物活性

THS-044 binding stabilizes the HIF2α PAS-B folded state, for regulating HIF2 activity in endogenous and clinical settings. Target: HIF2α Limited trypsin proteolysis reveals that both apo and THS-044-bound protein are efficiently cut at R330 in the extended HI loop. In the THS-044 bound state, there appears no additional proteolysis at the remaining candidate trypsin sites. In contrast, these THS-044-protected sites are protease accessible in the unliganded protein, leading its complete degradation. In parallel, NMR-based deuterium exchange measurements revealed a dramatic stabilization of the THS-044-bound protein β-sheet, with some sites experiencing 100-fold enhanced protection factors relative to the ligand-free protein.

分子量

291.23

Formula

C11H12F3N3O3
CAS 号

62054-67-5
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]. Motto I, et al. New aryl hydrocarbon receptor homology model targeted to improve docking reliability. J Chem Inf Model. 2011 Nov 28;51(11):2868-2881.

    [2]. Scheuermann TH, et al. Artificial ligand binding within the HIF2alpha PAS-B domain of the HIF2 transcription factor. Proc Natl Acad Sci U S A. 2009 Jan 13;106(2):450-455.

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m-PEG9-acid

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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。

m-PEG9-acid 

m-PEG9-acid 是一种 PROTAC linker，属于 PEG 类。可用于合成 PROTAC 分子。

m-PEG9-acid

m-PEG9-acid Chemical Structure

CAS No. : 2576495-35-5

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

m-PEG9-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

456.53

Formula

C20H40O11
CAS 号

2576495-35-5
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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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

UNC1079

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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。

UNC1079  纯度: ≥98.0%

UNC1079是UNC1021的哌啶类似物，结构相似，但具有较低的有效抑制剂用。

UNC1079

UNC1079 Chemical Structure

CAS No. : 1418741-86-2

规格 价格 是否有货 数量
5 mg ￥1300 In-stock
10 mg ￥2200 In-stock
25 mg ￥5000 In-stock
50 mg ￥8500 In-stock
100 mg ￥14500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

UNC1079 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library

生物活性

UNC1079 is the piperidine analog of UNC1021, as a structurally similar but significantly less potent inhibitor for use as a negative control in cellular studies. Target: L3MBTL3 The low anticipated affinity of UNC1079 was confirmed, as it demonstrated an activity versus L3MBTL3 of > 10 μM by AlphaScreen, which is >1000-fold weaker than UNC1215. UNC1079 also displays weak binding by ITC.

分子量

466.66

Formula

C28H42N4O2
CAS 号

1418741-86-2
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 : 2.22 mg/mL (4.76 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 2.1429 mL 10.7144 mL 21.4289 mL
5 mM — — —
10 mM — — —

*

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。
参考文献

  • [1]. James LI, et al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol. 2013 Mar;9(3):184-91.

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

m-PEG12-Mal

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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。

m-PEG12-Mal 

m-PEG12-Mal 是一种 PROTAC linker，属于 PEG 类。可用于合成 PROTAC 分子。

m-PEG12-Mal

m-PEG12-Mal Chemical Structure

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

m-PEG12-Mal is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

710.81

Formula

C32H58N2O15
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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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

Tafasitamab(Synonyms: XmAb5574; MOR00208; Tafasitamab-cxix)

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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。

Tafasitamab (Synonyms: XmAb5574; MOR00208; Tafasitamab-cxix)

Tafasitamab 是一种Fc修饰的人源化单克隆抗体，可与人B细胞表面抗原CD19结合。

Tafasitamab(Synonyms: XmAb5574; MOR00208; Tafasitamab-cxix)

Tafasitamab Chemical Structure

CAS No. : 1422527-84-1

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生物活性

Tafasitamab is an Fc-modified, humanized monoclonal antibody that binds to the human B-cell surface antigenCD19[1][2].

体外研究
(In Vitro)

Tafasitamab induces cytotoxicity against Mino and Jeko (MCL) cell lines in an E/T ratio-dependent manner XmAb5574 increases ADCP and antiproliferative activity. Tafasitamab (XmAb5574) enhances antiproliferative apoptotic activity due to caspase-induced apoptosis[1][2].

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

Cell Cytotoxicity Assay[1]

Cell Line: NHL cell lines and primary CLL and MCL cells by γδ T cells
Concentration:
Incubation Time: 2 h
Result: Induced killing of NHL cell lines and primary CLL and MCL cells by γδ T cells.

Cell Proliferation Assay[2]

Cell Line: SU-DHL-6 cells
Concentration:
Incubation Time: 72 h
Result: Showed potent antiproliferative effects on tumor cell.

Apoptosis Analysis[2]

Cell Line: SU-DHL-6 cells
Concentration: 0-4 ng/mL
Incubation Time: 48 h
Result: Showed potent antiproliferative effects due to caspase-induced apoptosis

体内研究
(In Vivo)

Tafasitamab (SC, once on Day 1, 2.5 μg/kg) inhibits lymphoma growth in disseminated BL mouse xenograft tumor models[1].

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

Animal Model: Disseminated Raji model[1].
Dosage: 2.5 μg/kg
Administration: Tafasitamab (SC, once on Day 1, 2.5 μg/kg)
Result: Showed antitumor activity in disseminated Raji model.
Animal Model: Disseminated Ramos model[1].
Dosage: 10 mg/kg
Administration: Tafasitamab (IV, on Days 3, 6, 10, 13, 17, and 20 at a dose of 10 mg/kg)
Result: Showed antitumor activity in disseminated Ramos model.

CAS 号

1422527-84-1
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]. Jung Hyun Her, et al. Tafasitamab mediates killing of B-cell non-Hodgkin’s lymphoma in combination with γδ T cell or allogeneic NK cell therapy. Cancer Immunol Immunother. 2022 Mar 29.

    [2]. Holly M Horton, et al. Potent in vitro and in vivo activity of an Fc-engineered anti-CD19 monoclonal antibody against lymphoma and leukemia. Cancer Res

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Doxycycline calcium

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Doxycycline calcium 

Doxycycline calcium 是一种具有口服活性的四环素抗生素，是广谱的金属蛋白酶 (MMP) 抑制剂，具有抗菌活性和抗癌细胞增殖活性。

Doxycycline calcium

Doxycycline calcium Chemical Structure

CAS No. : 94088-85-4

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Doxycycline calcium 的其他形式现货产品:

Doxycycline Doxycycline (hyclate)

生物活性

Doxycycline calcium, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor[1]. Doxycycline calcium shows antibacterial activity and anti-cancer cell proliferation activity[1][2][3][4][5].

体外研究
(In Vitro)

Doxycycline calcium (0.01-10 µg/mL, 4 d) affects growth of glioma cells only under high concentrations[2].
Doxycycline calcium (0.01-10 µg/mL, 24 h) decreases MT-CO1 protein content with concentrations of 1 µg/mL and higher in SVG cells[2].
Doxycycline calcium (100 ng/mL, 1 µg/mL; 24 h) reduces proliferation of human cell lines[4].
Doxycycline calcium (0-250 μM, 72 h) inhibits cell viability of breast cancer cells [5].

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: LNT-229, G55, and U343 glioma cells
Concentration: 0.01, 0.1, 1 or 10 µg/mL
Incubation Time: 4 days
Result: Affected growth of glioma cells only under high concentrations.

Cell Viability Assay[2]

Cell Line: SVG cells
Concentration: 0.01, 0.1, 1 or 10 µg/mL
Incubation Time: 24 hours
Result: Decreaseed MT-CO1 protein content with concentrations of 1 µg/mL and higher.

Cell Proliferation Assay[4]

Cell Line: MCF 12A, 293T cells
Concentration: 100 ng/mL, 1 µg/mL
Incubation Time: 96 hours
Result: Caused reduced proliferation of MCF 12A and 293T cells at 1 µg/mL.

Cell Viability Assay[5]

Cell Line: MCF-7, MDA-MB-468 cells
Concentration: 0-250 μM
Incubation Time: 72 hours
Result: Inhibited breast cancer cells in a dose-dependent manner with IC50 values for MCF-7 and MDA-MB-468 of 11.39 μM and 7.13 μM respectively.

体内研究
(In Vivo)

Doxycycline calcium (oral gavage; 200 or 800 mg/kg; once daily; 3 months) reduces MMP-9 activity in untreated HT mice in a dose-dependent manner[3].

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

Animal Model: 6-month-old female Heterozygous Col3a1-deficient (HT) mice[3]
Dosage: 200 or 800 mg/kg
Administration: Oral gavage; 200 or 800 mg/kg; once daily; 3 months
Result: Reduced MMP-9 activity in a dose-dependent manner.

分子量

524.59

Formula

C22H24Ca2N2O8
CAS 号

94088-85-4
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.
参考文献

  • [1]. Eusebio Manchado, et al. A combinatorial strategy for treating KRAS-mutant lung cancer. Nature. 2016 Jun 30;534(7609):647-51.

    [2]. Anna-Luisa Luger, et al. Doxycycline Impairs Mitochondrial Function and Protects Human Glioma Cells from Hypoxia-Induced Cell Death: Implications of Using Tet-Inducible Systems. Int J Mol Sci. 2018 May 17;19(5):1504.

    [3]. Wilfried Briest, et al. Doxycycline ameliorates the susceptibility to aortic lesions in a mouse model for the vascular type of Ehlers-Danlos syndrome. J Pharmacol Exp Ther. 2011 Jun;337(3):621-7.

    [4]. Ethan Ahler, et al. Doxycycline alters metabolism and proliferation of human cell lines. PLoS One. 2013 May 31;8(5):e64561.

    [5]. Le Zhang, et al. Doxycycline inhibits the cancer stem cell phenotype and epithelial-to-mesenchymal transition in breast cancer. Cell Cycle. 2017 Apr 18;16(8):737-745.

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USP7-IN-3

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USP7-IN-3  纯度: 99.86%

USP7-IN-3 (Compound 5) 是一种有效的选择性变构型泛素特异性蛋白酶7 (USP7) 抑制剂。

USP7-IN-3

USP7-IN-3 Chemical Structure

CAS No. : 2202738-42-7

规格 价格 是否有货 数量
1 mg ￥3800 In-stock
5 mg ￥12000 In-stock
10 mg ￥19500 In-stock
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100 mg   询价  

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USP7-IN-3 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor[1].

IC50 & Target

USP7[1]
分子量

568.59

Formula

C29H31F3N6O3
CAS 号

2202738-42-7
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 : 90 mg/mL (158.29 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7587 mL 8.7937 mL 17.5874 mL
5 mM 0.3517 mL 1.7587 mL 3.5175 mL
10 mM 0.1759 mL 0.8794 mL 1.7587 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: ≥ 4.5 mg/mL (7.91 mM); Clear solution

    此方案可获得 ≥ 4.5 mg/mL (7.91 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 45.0 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: ≥ 4.5 mg/mL (7.91 mM); Clear solution

    此方案可获得 ≥ 4.5 mg/mL (7.91 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 45.0 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]. Gavory G, et al. Discovery and characterization of highly potent and selective allosteric USP7 inhibitors. Nat Chem Biol. 2018 Feb;14(2):118-125.

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m-PEG36-alcohol

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m-PEG36-alcohol 

m-PEG36-alcohol 是一种 PROTAC linker，属于 PEG 类。可用于合成 PROTAC 分子。

m-PEG36-alcohol

m-PEG36-alcohol Chemical Structure

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生物活性

m-PEG36-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

1618.00

Formula

C3H8O2
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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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Indigo(Synonyms: 靛青)

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Indigo (Synonyms: 靛青) 纯度: ≥98.0%

Indigo 是一种深色吲哚基团染料，可从 Indigofera tinctoria 和相关物种中分离得到。

Indigo(Synonyms: 靛青)

Indigo Chemical Structure

CAS No. : 482-89-3

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
100 mg ￥500 In-stock
200 mg   询价  
500 mg   询价  

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Indigo 相关产品

•相关化合物库:

  • Natural Product Library Plus
  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus

生物活性

Indigo is a deep and rich color dye for indole stain, isolated from the plant Indigofera tinctoria and related species[1].

Clinical Trial

分子量

262.26

Formula

C16H10N2O2
CAS 号

482-89-3
中文名称

靛青
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 : < 1 mg/mL (insoluble or slightly soluble)

H2O : < 0.1 mg/mL (insoluble)
参考文献

  • [1]. Maerz and Paul A Dictionary of Color New York:1930 McGraw-Hill Page 197; Color Sample of Indigo: Page 117 Plate 47 Color Sample E10.

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Deltasonamide 2

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Deltasonamide 2 

Deltasonamide 2 是一种竞争性的，高亲和力的 PDEδ 抑制剂，Kd 值约为 385 pM。

Deltasonamide 2

Deltasonamide 2 Chemical Structure

CAS No. : 2088485-34-9

规格 价格 是否有货
5 mg ￥3500 询问价格 & 货期
10 mg ￥5500 询问价格 & 货期
50 mg ￥16500 询问价格 & 货期

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Deltasonamide 2 的其他形式现货产品:

Deltasonamide 2 (TFA) Deltasonamide 2 hydrochloride

生物活性

Deltasonamide 2 is a competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM[1].

IC50 & Target

Kd: ~385 pM (PDEδ)[1]
分子量

647.25

Formula

C30H39ClN6O4S2
CAS 号

2088485-34-9
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.
参考文献

  • [1]. Klein CH, et al. PDEδ inhibition impedes the proliferation and survival of human colorectal cancer cell linesharboring oncogenic KRas. Int J Cancer. 2019 Feb 15;144(4):767-776.

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Tos-PEG9-Tos

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Tos-PEG9-Tos 

Tos-PEG9-Tos 是一种 PROTAC linker，属于 PEG 类。可用于合成 PROTAC 分子。

Tos-PEG9-Tos

Tos-PEG9-Tos Chemical Structure

CAS No. : 109635-64-5

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

Tos-PEG9-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

722.86

Formula

C32H50O14S2
CAS 号

109635-64-5
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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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m-PEG8-Mal

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m-PEG8-Mal 

m-PEG8-Mal 是一种 PROTAC linker，属于 PEG 类。可用于合成 PROTAC 分子。

m-PEG8-Mal

m-PEG8-Mal Chemical Structure

CAS No. : 1334169-90-2

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

m-PEG8-Mal is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

534.60

Formula

C24H42N2O11
CAS 号

1334169-90-2
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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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Aristolochic acid D

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Aristolochic acid D  纯度: 98.55%

Aristolochic acid D 是从 Aristolochia indica 分离得到的马兜铃酸衍生物。马兜铃酸是肾毒素和致癌物。

Aristolochic acid D

Aristolochic acid D Chemical Structure

CAS No. : 17413-38-6

规格 价格 是否有货 数量
1 mg ￥2290 In-stock
5 mg ￥6860 In-stock
10 mg   询价  
50 mg   询价  

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Aristolochic acid D 相关产品

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生物活性

Aristolochic acid D is an aristolochic acid derivative isolated from stems of Aristolochia indica. Aristolochic acid is nephrotoxin and carcinogen[1].

分子量

357.27

Formula

C17H11NO8
CAS 号

17413-38-6
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
参考文献

  • [1]. Kupchan SM, et al. The isolation and structural elucidation of novel derivatives of aristolochic acid from Aristolochia indica. J Org Chem. 1968 Oct;33(10):3735-8.

    [2]. Balachandran P, et al. Structure activity relationships of aristolochic acid analogues: toxicity in cultured renal epithelial cells. Kidney Int. 2005 May;67(5):1797-805.

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MSC-4106

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MSC-4106 

MSC-4106 是一种具有口服活性的 YAP/TAZ-TEAD 抑制剂。 MSC-4106 阻断 TEAD1 和 TEAD3 的 auto-palmitoylation，对 NCI-H226 异种移植瘤模型具有抑制作用。

MSC-4106

MSC-4106 Chemical Structure

CAS No. : 2738542-58-8

规格 是否有货
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生物活性

MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model[1].

体外研究
(In Vitro)

MSC-4106 (10 μM, 24 h) inhibited SK-HEP-1 reporter and NCI-266 cell viability with IC50 values of 4 nM and 14 nM, respectively[1].
MSC-4106 (10 μM, 6 h) crystallizes in the P-site of TEAD1, and against TEAD1 or TEAD3 palmitoylation in TEAD-Overexpressing HEK293 Cells by 97.3% and 75.9%, respectively[1].
MSC-4106 (10 μM, 4 d) targets TEAD indicated by a reduction in viability of NCI-H226 cells[1].

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

Cell Viability Assay[1]

Cell Line: NCI-H226 (YAP dependent); SW620 YAP/TAZ KO (Yap-independent) cells
Concentration: 0, 3, 6, 9, 12, 15, 18, 21, 24, 26, 30 μM
Incubation Time: 96 hours
Result: Showed inhibitory effect to NCI-H226 and general cytotoxic to SW620 (IC50 >30 μM).

Immunofluorescence[1]

Cell Line: SK-HEP-1
Concentration: 0, 3, 6, 9, 12, 15, 18, 21, 24, 26, 30 μM
Incubation Time: 24 hours
Result: Inhibited YAP-TEAD interation.

体内研究
(In Vivo)

MSC-4106 (P.O.; 100 mg/kg once daily; 7 days) displays anti-tumor effect with controlled tumor volume and good tolerability with stable body weight in mice[1].
MSC-4106 (P.O.; 1, 5, 100 mg/kg once daily; 6, 24, 30, 48, and 72 h) down-regulates Cyr61 (cysteine-rich angiogenic inducer 61) expression, the TEAD-regulated target gene, in tumor lysates at all time points at 100 mg/kg and 24 h at 5 mg/kg[1].
Pharmacokinetics (PK) profile in different species[1]

Parameter Mouse Rat Dog
Cl (l/h/kg) 0.2 0.7 0.05
PO t1/2 (h) 45 40 3.6
PO AUC (μg•h/mL) 45 10 33
Vss (L/kg) 2 5 0.3
F (%) >90 80 18

Note: PO studies were performed at 10 mg/kg; MSC-4106 was formulated in 20% Kleptose in 50 mM PBS at pH 7.4.

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

Animal Model: NCI-H226 xenograft model in H2d Rag2 female mice (9-week-old)[1]
Dosage: 5, 100 mg/kg
Administration: Oral gavage; once daily; 32 days
Result: Resulted tumor growth controlled with 5 mg/kg while regressed with 100 mg/kg dosing after 32 treatment days.

分子量

359.30

Formula

C18H12F3N3O2
CAS 号

2738542-58-8
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]. Timo Heinrich, et al. Optimization of TEAD P-site binding fragment hit into in vivo active lead MSC-4106. J. Med. Chem. 2022, 65, 13, 9206–9229.

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