MS-275 (Entinostat) | HDAC inhibitor
NMR (Conforms)
Available Options
| Size | Price | Quantity | |
|---|---|---|---|
| 5 mg | $50.00 | ||
| 25 mg | $160.00 |
MS-275 (Entinostat 209783-80-2) is a potent HDAC inhibitor. Selective for HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 μM) and HDAC8 (IC50 100 μM).1 In vivo, MS-275, has been shown to inhibit tumor growth via induction of the tumor suppressors p21WAF1/CIP1 and gelsolin2 and to block cell proliferation in a variety of cancer cell lines. MS-275 has also shown significant anti-rheumatic activity in rat and mouse arthritis models.5
References/Citations:
1) Hu et al. (2003), Identification of novel isoform-selective inhibitors within class 1 histone deacetylases; J. Pharmacol. Exp. Ther., 307 720
2) Saito et al. (1999), A synthetic inhibitor of histone deacetylase, MS-275, with marked in vivo antitumor activity against human tumors; Proc. Natl. Acad. Sci. USA, 96 4592
3) Eyupoglu et al. (2006), Experimental therapy of malignant gliomas using the inhibitor of histone deacetylase MS-275; Mol. Cancer Ther., 5 1248
4) Lee et al. (2001), MS-275, a histone deacetylase inhibitor, selectively induces transforming growth factor beta type II receptor expression in human breast cancer cells; J. Pharmacol. Exp. Ther., 307 720
5) Lin et al. (2007), Anti-rheumatic activities of histone deacetylase (HDAC) inhibitors in vivo in collagen-induced arthritis in rodents; Br. J. Pharmacol., 150 862
6) Fukuchi et al. (2015), Class I histone deacetylase-mediated repression of the proximal promoter of the Activity-regulated Cytoskeleton-associated Protein Gene regulates its response to brain-derived neurotrophic factor; J. Biol. Chem. 290 6825 [Focus Biomolecules Citation]
NMR (Conforms)
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Product Data Sheet:
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MS-275 (Entinostat 209783-80-2) is a potent HDAC inhibitor. Selective for HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 μM) and HDAC8 (IC50 100 μM).1 In vivo, MS-275, has been shown to inhibit tumor growth via induction of the tumor suppressors p21WAF1/CIP1 and gelsolin2 and to block cell proliferation in a variety of cancer cell lines. MS-275 has also shown significant anti-rheumatic activity in rat and mouse arthritis models.5
References/Citations:
1) Hu et al. (2003), Identification of novel isoform-selective inhibitors within class 1 histone deacetylases; J. Pharmacol. Exp. Ther., 307 720
2) Saito et al. (1999), A synthetic inhibitor of histone deacetylase, MS-275, with marked in vivo antitumor activity against human tumors; Proc. Natl. Acad. Sci. USA, 96 4592
3) Eyupoglu et al. (2006), Experimental therapy of malignant gliomas using the inhibitor of histone deacetylase MS-275; Mol. Cancer Ther., 5 1248
4) Lee et al. (2001), MS-275, a histone deacetylase inhibitor, selectively induces transforming growth factor beta type II receptor expression in human breast cancer cells; J. Pharmacol. Exp. Ther., 307 720
5) Lin et al. (2007), Anti-rheumatic activities of histone deacetylase (HDAC) inhibitors in vivo in collagen-induced arthritis in rodents; Br. J. Pharmacol., 150 862
6) Fukuchi et al. (2015), Class I histone deacetylase-mediated repression of the proximal promoter of the Activity-regulated Cytoskeleton-associated Protein Gene regulates its response to brain-derived neurotrophic factor; J. Biol. Chem. 290 6825 [Focus Biomolecules Citation]
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