产品
编 号:F741459
分子式:C32H32N6O2
分子量:532.64
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性:
CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12.

体外研究:
CDK12-IN-2 在低亚微摩尔浓度下抑制 SK-BR-3 细胞中 CTD Ser2 的磷酸化,它抑制 C-末端结构域 ser2 磷酸化,IC50 为 185 nM。CDK12-IN-2 对 SK-BR-3 细胞具有生长抑制作用,IC50 为 0.8 μM。CDK12-IN- 2 显示 CDK12 抑制的时间依赖性,CDK12-IN-2 的 IC50 值分别为 0.0078 μM、0.042 μM、0.057 μM 和 0.059 μM,分别为 0h、1h、2h 和 5h。
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