Entinostat (MS275; SNDX275)

Description: Entinostat (formerly known as MS-275; SNDX-275) is a potent, benzamide-based and class-selective but generally pan-HDAC (histone deacetylase) inhibitor with potential anticancer activity. It strongly inhibits HDAC1, HDAC2 and HDAC3 with IC50 of 0.24, 0.45, 0.25 uM in cell-free assays respectively, it is more selective for HDAC1/2/3 over HDACs 4, 6, 8, and 10. Entinostat has potential anticancer activity by binding to and inhibiting histone deacetylase, an enzyme that regulates chromatin structure and gene transcription. This agent appears to exert dose-dependent effects in human leukemia cells including cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1)-dependent growth arrest and differentiation at low drug concentrations.

References: Proc Natl Acad Sci U S A. 1999 Apr 13; 96(8):4592-7; Neuroscience. 2010 Aug 11; 169(1):370-7; Clin Cancer Res. 2007 Aug 1; 13(15 Pt 1):4538-46.