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BIOLOGICAL INFO
Solubility:
DMSO
Application(s):
HDAC1 and HDAC3 inhibitor
Form:
Free base
Research Area:
Cancer
REVIEW Entinostat, also known as SNDX-275 and MS-275, is a benzamide histone deacetylase inhibitor undergoing clinical trials for treatment of various cancers. Entinostat inhibits class I HDAC1 and HDAC3 with IC50 of 0.51uM and 1.7 uM, respectively. Entinostat is a well-tolerated HDAC inhibitor that demonstrates promising therapeutic potential in both solid and hematologic malignancies. Histone deacetylases (EC 3.5.1.98, HDAC) are a class of enzymes that remove acetyl groups (O=C-CH3) from an epsilon-N-acetyl lysine amino acid on a histone, allowing the histones to wrap the DNA more tightly. This is important because DNA is wrapped around histones, and DNA expression is regulated by acetylation and deacetylation
REFERENCES
[1]
Hess-Stumpp H, Bracker TU, Henderson D, Politz O. MS-275, a potent orally available inhibitor of histone deacetylases--the development of an anticancer agent. Int J Biochem Cell Biol. 2007;39(7-8):1388-405.
[2]
Bracker TU, Sommer A, Fichtner I, Faus H, Haendler B, Hess-Stumpp H. fficacy of MS-275, a selective inhibitor of class I histone deacetylases, in human colon cancer models. Int J Oncol. 2009 Oct;35(4):909-20.
[3]
Knipstein J, Gore L. Einostat for treatment of solid tumors and hematologic malignancies. Expert Opin Investig Drugs. 2011 Oct;20(10):1455-67.
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