YJZ5118

Chemical Structure : YJZ5118

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货号: PC-24231Not For Human Use, Lab Use Only.

YJZ5118 is a potent, highly selective covalent inhibitor of CDK12/13 with IC50 of 39.5/26.4 nM, respectively, demonstrates high selectivity over other CDKs.

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生物&药学活性

YJZ5118 is a potent, highly selective covalent inhibitor of CDK12/13 with IC50 of 39.5/26.4 nM, respectively, demonstrates high selectivity over other CDKs.
YJZ5118 potently suppresses VCaP cell growth with an IC50 value of 23.7 nM.
YJZ5118 covalently binds with Cys1039 of CDK12.
YJZ5118 (100 nM) inhibits the phosphorylation of RNA polymerase II at Ser2 in VCaP cells, also has significant inhibitory effects on the expression of downstream gene RAD51 and markedly increaseds apoptotic marker c-PARP.
YJZ5118 not only provokes Akt phosphorylation but also exhibits a synergistic antitumor effect when combined with Akt inhibitors.

物理化学性质&存储条件

分子量	620.80
分子式	C36H44N8O2
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(5-(3-Benzyl-1-((1R,4R)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)ureido)-2-(4-(dimethylamino)piperidin-1-yl)phenyl)acrylamide

参考文献

1. Yang J, et al. J Med Chem. 2025 Mar 13. doi: 10.1021/acs.jmedchem.5c00127.

YJZ5118

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物理化学性质&存储条件

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YJZ5118

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物理化学性质&存储条件

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