Entinostat

Entinostat preferentially inhibits HDAC1 (IC50=300nM) over HDAC3 (IC50=8µM) and has no inhibitory activity towards HDAC8 (IC50>100µM). MS-275 induces cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1), slowing cell growth, differentiation, and tumor development in vivo. Recent studies suggest that MS-275 may be particularly useful as an antineoplastic agent when combined with other drugs, like adriamycin.

Entinostat

Synonyms: SNDX-275; MS-275; MS-27-275; Entinostat; pyridin-3-ylmethyl 4-(2-aminophenylcarbamoyl)benzylcarbamate
Technical Data: Molecular Weight - 376.42; Molecular formula - C21H20N4O3; CAS No - 209783-80-2

Ordering Information: Product Number - EC-000.2117
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References:
1. Saito, A. et al. A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. Proc Natl Acad Sci USA 96 4592-4597 (1999).
2. Jaboin, J., et al. MS-27-275, an inhibitor of histone deacetylase, has marked in vitro and in vivo antitumor activity against pediatric solid tumors. Cancer Res 62 6108-6115 (2002).
3. Rosato RR, et al. The histone deacetylase inhibitor MS-275 promotes differentiation or apoptosis in human leukemia cells through a process regulated by generation of reactive oxygen species and induction of p21CIP1/WAF1 1. Cancer Res 2003; 63: 3637-3645.

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Related service: collection of Histone Deacetylase Inhibitors.