E966-0530-45418

Chemical Structure : E966-0530-45418

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货号: PC-23770Not For Human Use, Lab Use Only.

E966-0530-45418 is a potent, selective inhibitor of CDK8 with IC50 of 129 nM, shows slightly weaker activity against CDK19 and does not inhibit other CDKs.

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生物&药学活性

E966-0530-45418 is a potent, selective inhibitor of CDK8 with IC50 of 129 nM, shows slightly weaker activity against CDK19 and does not inhibit other CDKs.
E966-0530-45418 significantly inhibits the phosphorylation of STAT1 at Ser727 in a concentration-dependent manner without affecting CDK8 expression in DU145 and PC-3 cells transfected with pcDNA3 CDK8-HA plasmid.
E966-0530-45418 significantly inhibits cell migration and the expression of EMT proteins in prostate cancer cells.
E966-0530-45418 suppresses TGF-β1/Smad signaling through inhibition of RNA polymerase II and Smad linker phosphorylation, inhibits β-catenin signaling and downstream proteins via CDK8 inhibition.
E966-0530-45418 (50 mg/kg, q.d., oral) exhibits antimetastatic properties in PC-3 SCID mouse model.

物理化学性质&存储条件

分子量	496.51
分子式	C24H21FN4O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(3-fluoro-4-((2-oxo-3-(propan-2-ylidene)indoline)-5-sulfonamido)phenoxy)-N-methylpicolinamide

参考文献

1. Ho TY, et al. Biomed Pharmacother. 2023 Jun;162:114667.

E966-0530-45418

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物理化学性质&存储条件

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E966-0530-45418

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