CDK-IN-9 (compound 24) 是一种有效的CDK抑制剂，也作为一个分子胶诱导 CDK12 和 DDB1 的互作，对 CDK2/E 的IC50为 4 nM。CDK-IN-9 导致细胞周期蛋白 K (cyclin K) 的多泛素化及其随后的降解。CDK-IN-9 通过去磷酸化视网膜母细胞瘤蛋白和RNA 聚合酶 II诱导细胞凋亡 (Apoptosis)。

CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC 50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II [1].

CDK-IN-9 (compound 24) (0.005, 0.05, 0.5, or 5 μM; 2 h) potently decreases the level of cyclin K in MINO cells at 5 nM, and makes cyclin K disappear completely at 50 nM [1]. CDK-IN-9 makes siRNA silencing of DDB1 effectively stabilizes cyclin K at the protein level in treated MINO cells [1]. CDK-IN-9 (2.5-40 nM; 24 h) activates caspases 3/7/9 and decreases anti-apoptotic proteins Mcl-1 and XIAP in MINO cells [1].

CDK-IN-9 (0.1-10 mg/kg; IP, single dosage) causes the decrease in cyclin K and CDK12 levels [1].

C21H24N8S

420.53

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years