MS-275 (Entinostat) | HDAC inhibitor

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]