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HDAC1 inhibitor
Preferentially inhibits HDAC1 (IC50=300nM) over HDAC3 (IC50=8µM). Has no inhibitory activity towards HDAC8 (IC50>100µM).
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Product Details
| Alternative Name |
N-(2-Aminophenyl)-4-[N-(pyridine-3-ylmethoxy-carbonyl)aminomethyl]benzamide, Entinostat |
|---|---|
| Appearance |
Off-white to tan solid. |
| CAS |
209783-80-2 |
| Couple Target |
HDAC, HDAC1 |
| Couple Type |
Inhibitor |
| Formula |
C21H20N4O3 |
| MW |
376.4 |
| Purity |
≥95% (1H-NMR) |
| Solubility |
Soluble in DMSO or methanol. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. |
|---|---|
| Handling |
Protect from light. Packaged under inert gas. |
| Long Term Storage |
-20°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- CDKN1A is a target for phagocytosis-mediated cellular immunotherapy in acute leukemia: Allouch, A., Voisin, L., et al.; Nat. Commun. 13, 6739 (2022), Abstract
- Liver disease–associated keratin 8 and 18 mutations modulate keratin acetylation and methylation: K. Jang, et al.; FASEB J. 33, 9030 (2019), Abstract — Full Text
- 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
- AF4 and AF4-MLL mediate transcriptional elongation of 5-lipoxygenase mRNA by 1, 25-dihydroxyvitamin D3: Ahmad, K., Scholz, B., et al.; Oncotarget 6, 25784 (2015), Abstract
- 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
- The anti-tumor effect of HDAC inhibition in a human pancreas cancer model is significantly improved by the simultaneous inhibition of cyclooxygenase 2: Peulen, O., Gonzalez, A., et al.; PLoS One 8, e75102 (2013), Abstract
- 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), Application(s): Inhibition, Abstract — Full Text
- HDAC2 regulates atypical antipsychotic responses through the modulation of mGlu2 promoter activity: Kurita, M., Holloway, T., et al.; Nat. Neurosci. 15, 1245 (2012), Abstract
- Expression of αB-crystallin overrides the anti-apoptotic activity of XIAP: Lee, J. S., Kim, H. Y., et al.; Neuro Oncol. 14, 1332 (2012), Abstract
- Vorinostat synergises with capecitabine through upregulation of thymidine phosphorylase: Di Gennaro, E., Piro, G., et al.; Br. J. Cancer 103, 1680 (2010), Abstract
- Histone deacetylase inhibitor MS-275 alone or combined with bortezomib or sorafenib exhibits strong antiproliferative action in human cholangiocarcinoma cells: Baradari, V., Höpfner, M., et al.; World J. Gastroenterol. 13, 4458 (2007), Abstract
- Antiproliferative and proapoptotic effects of histone deacetylase inhibitors on gastrointestinal neuroendocrine tumor cells: Baradari, V., Huether, A., et al.; Endocr. Relat. Cancer 13, 1237 (2006), Abstract
- 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
- 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
- Identification of novel isoform-selective inhibitors within class I histone deacetylases: E. Hu, et al.; Pharmacol Exp. Ther. 307, 720 (2003), Abstract
- 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-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
- 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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