gsk2801

Description: GSK2801 (GSK-2801) is a novel, orally bioavailable, selective, cell bioactive and acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains, which are the two closely related bromodomain containing proteins BAZ2A and BAZ2B constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC) that regulates the expression of noncoding RNAs. GSK2801 inhibits BAZ2A and BAZ2B with Kd of 257 nM and 136 nM, respectively. It has the potential to be used as a versatile tool compound for cellular and in vivo studies to understand the role of BAZ2 bromodomains in chromatin biology.

References: J Med Chem. 2016 Feb 25; 59(4):1410-24.

GSK-2801; GSK 2801; GSK2801

Chemical Name: 1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone

InChi Key: KHWCPNJRJCNVRI-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H21NO4S/c1-4-11-25-15-9-10-21-18(14(2)22)13-17(19(21)12-15)16-7-5-6-8-20(16)26(3, 23)24/h5-10, 12-13H, 4, 11H2, 1-3H3

SMILES Code: CC(C1=CC(C2=CC=CC=C2S(=O)(C)=O)=C3C=C(OCCC)C=CN13)=O