Preferentially inhibits HDAC1 (IC50=300nM) over HDAC3 (IC50=8µM). Has no inhibitory activity towards HDAC8 (IC50>100µM).
Product Details
Alternative Name: | N-(2-Aminophenyl)-4-[N-(pyridine-3-ylmethoxy-carbonyl)aminomethyl]benzamide, Entinostat |
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Formula: | C21H20N4O3 |
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MW: | 376.4 |
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CAS: | 209783-80-2 |
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Purity: | ≥95% (1H-NMR) |
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Appearance: | Off-white to tan solid. |
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Solubility: | Soluble in DMSO or methanol. |
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Shipping: | Ambient Temperature |
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Long Term Storage: | -20°C |
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Handling: | Protect from light. Packaged under inert gas. |
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Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Liver disease–associated keratin 8 and 18 mutations modulate keratin acetylation and methylation: K. Jang, et al.; FASEB J.
33, 9030 (2019),
Abstract;
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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
Inhibition of class I HDACs abrogates the dominant effect of MLL-AF4 by activation of wild-type MLL: K. Ahmad, et al.; Oncogenesis
3, e127 (2014),
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;
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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;
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