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CDK-IN-9
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CDK-IN-9图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)。
生物活性

CDK-IN-9 (compound 24) is a potentCDKinhibitor, also as a molecular glue inducing an interaction betweenCDK12and DDB1, with anIC50values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induceapoptosisthrough dephosphorylation of retinoblastoma protein andRNA polymerase II[1].

IC50& Target[1]

CDK2/E

4 nM (IC50)

Cdk5/p25

39 nM (IC50)

CDK9/T1

20 nM (IC50)

CDK12/K

64 nM (IC50)

CDK13/K

22 nM (IC50)

体外研究
(In Vitro)

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].

体内研究
(In Vivo)

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

分子量

420.53

Formula

C21H24N8S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.