SKLB-03176 | EZH2 covalent inhibitor | Probechem Biochemicals

Chemical Structure : SKLB-03176

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SKLB-03176 (SKLB03176)

货号: PC-72287Not For Human Use, Lab Use Only.

SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.

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生物&药学活性

SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.
SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N, and EZH2A677G at 200 nM concentration.
SKLB-03176 exhibited weak activity against other targets, such as 5 histone methyltransferases and more than 30 kinases, >50-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 (IC50=2.45 uM).
SKLB-03176 inhibited the activity of a variety of EZH2 mutants and significantly inhibited the expression of H3K27Me3 in cells.
SKLB-03176 showed no cytotoxicity to normal cells.

物理化学性质&存储条件

分子量	514.63
分子式	C29H34N6O3
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	3-acrylamido-N-((4-ethyl-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-5-(6-(piperazin-1-yl)pyridin-3-yl)benzamide

参考文献

1. Zhang Q, et al. Biomed Pharmacother. 2022 Mar;147:112617.

SKLB-03176 (SKLB03176)

生物&药学活性

物理化学性质&存储条件

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SKLB-03176 (SKLB03176)

生物&药学活性

物理化学性质&存储条件

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