MS-275

Aliases: Entinostat, Pyridin-3-ylmethyl 4-((2-aminophenyl)carbamoyl)benzylcarbamate
Catalog No: 14042 Format: 25 mg $200 Buy
Catalog No: 14043 Format: 5 mg $60 Buy
Application: Histone Acetylation (HAT & HDAC)

Chemical Properties

MW = 376.4
C21H20N4O3
CAS 209783-80-2
≥98% (TLC); NMR (Conforms)

Description

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 M); HDAC3 (IC50 = 8 M) with no inhibition of HDAC 8 (at > 100 M) (ref 1). Induces hyperacetylation of nuclear histones in tumor cells resulting in inhibition of proliferation of a variety of human tumor cell lines (ref 2). Protects p53-deficient mice against ischemic injury (ref 3). Suppresses the p38 MAP kinase pathway in rheumatoid arthritic synovial fibroblasts (ref 4). Active in vivo.

Contents

Pale yellow powder. May be dissolved in DMSO (25 mg/ml, warm).

Storage Conditions

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

References

1. E Hu et al. J. Pharmacol. Exp. Ther. 2003, 307:720
2. A Saito et al. Proc. Natl. Acad. Sci. USA 1999, 96:4592
3. SP Murphy et al. J. Neurochem. 2013, Oct 21 epub
4. QY Choo et al. Molecules 2013, 18:14085

 
Chemical structure of MS-275.

Chemical structure of MS-275.