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编 号:F762978
分子式:C21H24N8S
分子量:420.53
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生物活性:
CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 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.

体内研究:
CDK-IN-9 (0.1-10 mg/kg; IP, single dosage) causes the decrease in cyclin K and CDK12 levels.

体外研究:
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.CDK-IN-9 makes siRNA silencing of DDB1 effectively stabilizes cyclin K at the protein level in treated MINO cells.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.
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