LC-CE-7

Chemical Structure : LC-CE-7

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货号: PC-23888Not For Human Use, Lab Use Only.

LC-CE-7 is a potent, sepecific and allosteric covalent CECR2 inhibitor with IC50 of 462 nM and Ki of 32.5 nM, exhibits covalent binding to Cys494 and allosteric regulation of the Kac pocket.

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生物&药学活性

LC-CE-7 is a potent, sepecific and allosteric covalent CECR2 inhibitor with IC50 of 462 nM and Ki of 32.5 nM, exhibits covalent binding to Cys494 and allosteric regulation of the Kac pocket.
LC-CE-7 effectively inhibited CECR2 at 2.5 μM, but did not affect other BRD family members, exhibits minimal inhibition of other BRDs lacking cysteine residues, such as CBP, BRD2, and BPTF.
LC-CE-7 displays anti-proliferative activity against breast cancer cell MDA-MB-231 with IC50 of 9.04 uM, with weak activity against non-cancer cell HUVEC (IC50=32.8 uM).
LC-CE-7 directly binds to CECR2 at the cellular level in CETSA assays in intact MDA-MB-231 cells.

物理化学性质&存储条件

分子量	360.47
分子式	C19H24N2O3S
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	(E)-2-(4-((2-cyanovinyl)sulfonyl)phenyl)-N-cyclohexyl-2-methylpropanamide

参考文献

1. Tang CL, et al. Acta Pharmacol Sin. 2025 Jan 20. doi: 10.1038/s41401-024-01452-z.

LC-CE-7

生物&药学活性

物理化学性质&存储条件

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LC-CE-7

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物理化学性质&存储条件

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