MS-275
HDAC inhibitor / 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 supressors p21WAF1/CIP1 and gelsolin2 and to block cell proliferation in a variety of cancer cell lines3,4. The compound has also shown significant anti-rheumatic activity in rat and mouse arthritis models.5
Biochemicals & reagents
209783-80-2
Entinostat; SNDX-275
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-27-275, 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
-20°C
TARGET: Protein deacetylase -- PATHWAY: Chromatin; Posttranslational modification; Proliferation -- RESEARCH AREA: Epigenetics -- DISEASE AREA: Cancer; Inflammation