MC180295(Synonyms: (rel)-MC180295)

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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。

MC180295 (Synonyms: (rel)-MC180295) 纯度: 98.41%

MC180295 ((rel)-MC180295) 是一种有效、选择性的 CDK9-Cyclin T1 抑制剂，IC50 值为 5 nM，对其选择性至少是对其他 CDK 激酶 22 倍。MC180295 ((rel)-MC180295) 同时抑制 GSK-3α 和 GSK-3β。MC180295 具有的抗肿瘤活性。

MC180295(Synonyms: (rel)-MC180295)

MC180295 Chemical Structure

CAS No. : 2237942-08-2

规格 价格 是否有货 数量
5 mg ￥2200 In-stock
10 mg ￥3550 In-stock
25 mg ￥6650 In-stock
50 mg ￥11700 In-stock
100 mg   询价  
200 mg   询价  

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MC180295 相关产品

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生物活性

MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect[1].

IC50 & Target[1]

CDK9- Cyclin T1

5 nM (IC50)

CDK1-Cyclin B

138 nM (IC50)

cdk2-cyclin A

233 nM (IC50)

cdk2-cyclin E

367 nM (IC50)

CDK3-Cyclin E

399 nM (IC50)

CDK4-Cyclin D

112 nM (IC50)

cdk5-p35

159 nM (IC50)

cdk5-p25

186 nM (IC50)

cdk6-cyclin D3

712 nM (IC50)

CDK7-CycH/MAT1

555 nM (IC50)

体外研究
(In Vitro)

MC180295 is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs, such as CDK1-Cyclin B (IC50, 138 nM), CDK2-Cyclin A (IC50, 233 nM), CDK2-Cyclin E (IC50, 367 nM), CDK3-Cyclin E (IC50, 399 nM), CDK4-Cyclin D (IC50, 112 nM), CDK5-P35 (IC50, 159 nM), CDK5-P25 (IC50, 186 nM), CDK6-Cyclin D3 (IC50, 712 nM), and CDK7-CycH/MAT1 (IC50, 555 nM). MC180295 also inhibits GSK-3α and GSK-3β[1].
MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation[1].
MC180295 (0.1 μM) inhibits the proliferation in cancer 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.
体内研究
(In Vivo)

MC180295 (20 mg/kg, i.p., qod) inhibits significant anti-tumor activity in mice bearing SW48 cells, shows no inhibitory activity against human T cell growth in vivo[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

358.41

Formula

C17H18N4O3S
CAS 号

2237942-08-2
运输条件

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

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (279.01 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7901 mL 13.9505 mL 27.9010 mL
5 mM 0.5580 mL 2.7901 mL 5.5802 mL
10 mM 0.2790 mL 1.3951 mL 2.7901 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 (stored under nitrogen)。-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]. Zhang H, et al. Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer. Cell. 2018 Nov 15;175(5):1244-1258.e26.

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