Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T39752 |
CDK12-IN-2
CDK12 inhibitor 2,CDK12-IN-2 |
CDK | Cell Cycle/Checkpoint |
CDK12-IN-2 (CDK12 inhibitor 2) 是一种有效的选择性 CDK12 抑制剂,对 CDK12、CDK2、CDK7 和 CDK9 的 IC50 为 52 nM、>100 μM、>10 μM 和 16 μM。 CDK12-IN-2可用于研究CDK12的功能。 | |||
T9758 |
dCeMM3
2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide |
Others | Others |
dCeMM3 (2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide) 是一种胶降解剂,可以诱导 cyclin K 的泛素化和降解。机制是通过促进 CDK12-cyclin K 与 CRL4B 连接酶复合物的相互作用。 | |||
T40289 |
CDK12-IN-6
CDK12-IN-6 |
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CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1). | |||
T69931 |
MFH290
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MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation ... |