MS-275, also known as Entinostat, is an inhibitor of histone deacetylases (HDACs) and preferentially inhibits HDAC1 over HDAC3. It does not inhibit HDAC8 (IC50 > 100 µM). It 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, inhibitors of PARPs, or inhibitors of Hsp90.
≥99% by HPLC.
1. Hu., E. et al., J. Pharmacol. Exp. Ther. 2003; 307: 720-728.
2. Saito, A., et al., Proc. Natl. Acad. Sci. USA 1999; 96: 4592-4597.
3. Jaboin, J., et al., Cancer Res. 2002; 62: 6108-6115.
4. Xu, J. et al., Cancer Res. 2008; (68)16: 6718 – 6726.
5. Gaymes, T.J., et al., Haematologica 2009; 94: 638-646.
Application Reference:
Immune evasion by oncogenic proteins of acute myeloid leukemia (2014)
