Chemical Structure : LC-CE-7
CAS No.:
1365091-26-4
LC-CE-7
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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360.47
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Formula
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C19H24N2O3S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(E)-2-(4-((2-cyanovinyl)sulfonyl)phenyl)-N-cyclohexyl-2-methylpropanamide
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References
1. Tang CL, et al. Acta Pharmacol Sin. 2025 Jan 20. doi: 10.1038/s41401-024-01452-z.
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