CDK7/9-IN-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CDK7/9-IN-1 

CDK7/9-IN-1 是一种细胞周期蛋白依赖性激酶 7/9 (CDK7/9) 抑制剂。CDK7/9-IN-1 选择性抑制 CDK7。CDK7/9-IN-1 在非预孵育和预孵育 3 小时后抑制 CDK7,IC50 分别为 0.0656 μM 和 0.00574 μM。 CDK7/9-IN-1 在预孵育 3 小时后抑制 CDK9,IC50 为 2.14 μM。 CDK7/9-IN-1可用于癌症研究。

CDK7/9-IN-1

CDK7/9-IN-1 Chemical Structure

CAS No. : 2747919-19-1

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生物活性

CDK7/9-IN-1 is a cyclin-dependent kinases 7/9 (CDK7/9) inhibitor. CDK7/9-IN-1 selectively inhibits CDK7 over CDK9. CDK7/9-IN-1 inhibits CDK7 with IC50s of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. CDK7/9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. CDK7/9-IN-1 can be used for the research of cancer[1].

IC50 & Target[1]

CDK7

5.74-65.6 nM (IC50)

CDK9

2.14 μM (IC50)

体外研究
(In Vitro)

CDK7/9-IN-1 (example 8; 0.001-20 μM; 4 h) inhibits CDK7 with an relative IC50 of 0.0262 μM for phospho-carboxyl terminal domain (Rbp2) (Ser5) in HCT116 cells[1].
CDK7/9-IN-1 (0.001-20 μM; 4 h) inhibits CDK9 with an IC50 of 2.59 μM for phospho-carboxyl terminal domain (Rbp2) (Ser2) in HCT116 cells[1].
CDK7/9-IN-1 (0.001-20 μM; 4 h) inhibits cMyc with an relative IC50 of 0.0138 μM in HCT116 cells[1].
CDK7/9-IN-1 (20 μΜ, 2 μΜ, and 0.2 μΜ; 1 h) shows excellent selectivity against the 468 protein kinases panel. CDK7/9-IN-1 shows approximately 96% inhibition against CDK7[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

479.54

Formula

C24H32F3N5O2

CAS 号

2747919-19-1

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.

参考文献
  • [1]. Maria Carmen FERNANDEZ FIGUEROA, et al. Compounds useful for inhibiting cdk7. WO2021242602 A1.

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