JH-XI-10-02

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JH-XI-10-02 是一种基于 CDK8 抑制剂 JH-VIII-49 的 CDK8 PROTAC，可诱导 Jurkat 细胞中 CDK8 部分降解，IC50 为 159 nM。

JH-XI-10-02 is a CDK8 PROTAC based on the CDK8 inhibitor JH-VIII-49, induces partial degradation of CDK8 in Jurkat cells with IC50 of 159 nM.

Western Blot Analysis Cell Line:Jurkat cells Concentration:1 μM Incubation Time:6 and 24 hours Result:Partial degradation of CDK8 upon treatment for 6 h at a concentration of 1 μM. Significant degradation of CDK8 after treatment for 24 h at a concentration of 1 μM.Western Blot Analysis Cell Line:WT Molt4 and CRBN null Molt4 cells Concentration:0.1, 0.5, 1, 2, 5 μM Incubation Time:24 hours Result:Degradation of CDK8 at 5 μM in WT Molt4 cells. There were no degradation in CRBN null Molt4 cells at any concentration.

——

——

PROTACs

PROTAC

PROTAC

——

——

2209085-22-1

920.161

C53H69N5O9

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (108.68 mM)

CC12CCC(CC1CCC3C2CCC4(C3CCC4C5=CC6=C(C=C5)C=CN=C6)C)N(C)C(=O)CCOCCOCCOCCOCCNC7=CC=CC8=C7C(=O)N(C8=O)C9CCC(=O)NC9=O

1-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)-N-((3S,5S,8R,9S,10S,13S,14S,17S)-17-(isoquinolin-7-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-3,6,9,12-tetraoxapentadecan-15-amide

(-20℃)

With Ice Pack

≥ 2 years