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MC180295

CAS No. : 2237942-08-2

MCE 站：MC180295

产品活性：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。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

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.
MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation.
MC180295 (0.1 μM) inhibits the proliferation in cancer cells.

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.

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