Entinostat, Free Base (MS-27-275, MS 275-27, MS-275, Histone Deacetylase Inhibitor I, SNDX-275, CAS 209783-80-2), >99%

LC Laboratories' Product Number E-3866 - Entinostat, Free Base (MS-27-275, MS 275-27, MS-275, Histone Deacetylase Inhibitor I, SNDX-275, CAS 209783-80-2), >99% - for research use only. Entinostat is a synthetic benzamide derivative that inhibited partially purified human histone deacetylase (HDA) with an IC50 of 2 µM and induced hyperacetylation of nuclear histones in tumor cell lines. Entinostat inhibited the proliferation of various human tumor cell lines such as A2780, Calu-3, HL-60, and K562 (IC50 values were 0.0415 µM, 0.195 µM, 0.212 µM, and 0.589 µM, respectively). Entinostat also inhibited the growth of human tumor xenografts in nude mouse. Entinostat inhibits tumor growth by inducing tumor suppressors p21WAF1/CIP1 and gelsolin through acetylation of histones and changing the cell cycle distribution, decrease of S-phase cells and increase of G1-phase cells. Entinostat inhibited the proliferation of human breast cancer cells by inducing the expression of transforming growth factor (TGF)-β type II receptor (TβRII) mRNA, but not TGF-beta type I receptor mRNA. Entinostat inhibited the proliferation of four glioma cell lines (U87MG, C6, F98, and SMA-560) with an IC90 of 3.75 µM. Its antiproliferative effect was mediated by G0-G1 cell cycle arrest and apoptosis. The toxicities of entinostat in patients included infections and neurologic toxicity, fatigue, anorexia, nausea, vomiting, hypoalbuminemia, and hypocalcemia. Entinostat demonstrated dramatic anti-rheumatic activities in both mouse and rat collagen induced arthritis (CIA) models. The combination treatment of PC-3 prostate cancer cells or tumors with retinoic acid metabolism-blocking agent (RAMBA) VN/66-1 and entinostat resulted in a significant inhibition in cell proliferation and tumor volume compared with control and was more effective than either drug alone. Another CAS number previously assigned to entinostat, 442532-99-2, has been deleted by CAS and is no longer in use.

• Supplier: LC Laboratories
• Product #: E-3866
• Sku #: E-3866_25mg