MS-275

Pyridin-3-ylmethyl 4-((2-aminophenyl)carbamoyl)benzylcarbamate; Entinostat

MS-275 is a potent and selective non-hydroxamate HDAC inhibitor. Considered to be a class I selective inhibitor but displays some selectivity amongst class I members:HDAC1 (IC₅₀ = 0.3 mM); HDAC3 (IC₅₀ = 8 mM) with no inhibition of HDAC8 (at >100 mM)¹. Induces hyperacetylation of nuclear histones in tumor cells resulting in inhibition of proliferation of a variety of human tumor cell lines². Protects p53-deficient mice against ischemic injury³. Suppresses the p38 MAP kinase pathway in rheumatoid arthritic synovial fibroblasts⁴. Active in vivo.

Physical Properties: Pale yellow powder

MW=376.4 C₂₁H₂₀N₄O₃

Analysis: >98% (TLC); NMR (Conforms)

Solubilization: May be dissolved in DMSO (25 mg/ml, warm)

Storage: Store desiccated as supplied at -20°C for up to 1 year. Store solutions at -20°C for up to 1 week.