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MS-275

HDAC1 inhibitor
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Not sold in the U.S.
Preferentially inhibits HDAC1 (IC50=300nM) over HDAC3 (IC50=8µM). Has no inhibitory activity towards HDAC8 (IC50>100µM).

Product Specification

Alternative Name:N-(2-Aminophenyl)-4-[N-(pyridine-3-ylmethoxy-carbonyl)aminomethyl]benzamide, Entinostat
 
Formula:C21H20N4O3
 
MW:376.4
 
CAS:209783-80-2
 
Purity:≥95% (1H-NMR)
 
Appearance:Off-white to tan solid.
 
Solubility:Soluble in DMSO or methanol.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Handling:Protect from light. Packaged under inert gas.
 
270-378
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270-378

Product Literature References

Ionizing radiation induces immediate protein acetylation changes in human cardiac microvascular endothelial cells: Z. Barjaktarovic, et al.; J. Radiat. Res. 56, 623 (2015), Application(s): Cell Culture, Abstract; Full Text
Histone deacetylase (HDAC) 1 controls the expression of beta defensin 1 in human lung epithelial cells: K. Kallsen, et al.; PLoS One 7, e50000 (2012), Abstract; Full Text
Enhanced radiation-induced cell killing and prolongation of gammaH2AX foci expression by the histone deacetylase inhibitor MS-275: K. Camphausen, et al.; Cancer Res. 64, 316 (2004), Abstract;
Gene expression profiling of multiple histone deacetylase (HDAC) inhibitors: defining a common gene set produced by HDAC inhibition in T24 and MDA carcinoma cell lines: K.B. Glaser, et al.; Mol. Cancer Ther. 2, 151 (2003), Abstract;
Identification of novel isoform-selective inhibitors within class I histone deacetylases: E. Hu, et al.; Pharmacol Exp. Ther. 307, 720 (2003), Abstract;
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: R.R. Rosato, et al.; Cancer Res. 63, 3637 (2003), Abstract;
MS-27-275, an inhibitor of histone deacetylase, has marked in vitro and in vivo antitumor activity against pediatric solid tumors: J. Jaboin, et al.; Cancer Res. 62, 6108 (2002), Abstract; Full Text
Transcriptional regulation of the transforming growth factor beta type II receptor gene by histone acetyltransferase and deacetylase is mediated by NF-Y in human breast cancer cells: S.H. Park, et al.; J. Biol. Chem. 277, 5168 (2002), Abstract; Full Text
MS-275, a histone deacetylase inhibitor, selectively induces transforming growth factor beta type II receptor expression in human breast cancer cells: B.I. Lee, et al.; Cancer Res. 61, 931 (2001), Abstract; Full Text
A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors: A. Saito, et al.; PNAS 96, 4592 (1999), Abstract; Full Text

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