Colrestat

Chemical Structure : Colrestat

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货号: PC-25935Not For Human Use, Lab Use Only.

Colrestat is a potent, selective inhibitor of class I histone deacetylases (HDACs) with IC50 of 41.2 nM, 52.5 nM and 74.3 nM for HDAC1, HDAC2 and HDAC3 respectively.

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生物&药学活性

Colrestat is a potent, selective inhibitor of class I histone deacetylases (HDACs) with IC50 of 41.2 nM, 52.5 nM and 74.3 nM for HDAC1, HDAC2 and HDAC3 respectively.
Colrestat weakly inhibits HDAC10 (IC50=4261 nM) and shows no activity against HDAC5/6/11 (IC50>10 uM).
Colrestat induces H3K9 acetylation, p21 upregulation, and G2/M arrest in colorectal cancer (CRC) cells, shows strong antitumor efficacy in vivo in the CAM assay for both compounds even outperforming entinostat.

物理化学性质&存储条件

分子量	415.45
分子式	C24H21N3O4
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)-N-(2-aminophenyl)-4-((3-(benzo[d][1,3]dioxol-5-yl)acrylamido)methyl)benzamide

参考文献

1. Carullo G, et al. J Med Chem. 2026 Jan 4. doi: 10.1021/acs.jmedchem.5c02237.

Colrestat

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Colrestat

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