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Entinostat (MS-275) -- HDAC Inhibitor

Overview
Catalog # bs-60174c-5mg-solid
Product Name Entinostat (MS-275) -- HDAC Inhibitor
Specifications
Storage Buffer Powder
Storage Condition Store in dry, dark place at -20C for 1 year.
Target
Product Information Molecular Weight: 376.41

Formula: C21 H20 N4 O3

CAS Number: 209783-80-2

InChi Key: INVTYAOGFAGBOE-UHFFFAOYSA-N

InChi: InChI=1S/C21H20N4O3/c22-18-5-1-2-6-19(18)25-20(26)17-9-7-15(8-10-17)13-24-21(27)28-14-16-4-3-11-23-12-16/h1-12H,13-14,22H2,(H,24,27)(H,25,26)

Smiles: NC1C=CC=CC=1NC(=O)C1C=CC(CNC(=O)OCC2=CC=CN=C2)=CC=1

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years
Description Entinostat (MS-275) is a potent and selective HDAC inhibitor. It inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, but not the other HDACs 4, 6, 8, and 10 (IC50 > 100 µM). MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. It was shown to reduce S-phase cells and induce G1-phase cells in A2780 cells. MS-275 shows great inhibition to human leukemia and lymphoma cells, decreases expression of cyclin D1 and the anti-apoptotic proteins Mcl-1 and XIAP. In vivo MS-275 exhibits great antitumor activity against human tumor xenografts. Currently it is in Phase II/III clinical trials for Hodgkin's lymphoma and advanced breast cancer.