GSK343

Description: GSK343 is a novel, highly potent and selective inhibitor of H3-lysine 27 (H3K27) methyltransferase EZH2 with antineoplastic activity. It inhibits EZH2 with an IC50 of 4 nM in a cell-free assay, and displays > 60 fold selectivity for EZH2 over EZH1, and other histone methyltransferases. GSK343 was found to inhibit cell proliferation in some breast and prostate cancer cells. In LNCaP cells, GSK343 suppressed cell growth with IC50 value of 2.9 uM. In human EOC cells, GSK343 notably inhibited cell invasion and induced cell apoptosis. GSK343 was also found to induce LC3-II accumulation and autophagy in A549, MDA-MB-231 and HepG2 cell.

References: ACS Med Chem Lett. 2012, 3, 1091-1096; Cell Cycle. 2013 Jul 1; 12(13):2113-9.

GSK-343; GSK 343; GSK343

Chemical Name: 1-isopropyl-N-((6-methyl-2-oxo-4-propyl-1, 2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-1H-indazole-4-carboxamide.

InChi Key: ULNXAWLQFZMIHX-UHFFFAOYSA-N

InChi Code: InChI=1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9, 14-17, 19-20H, 6-7, 10-13, 18H2, 1-5H3, (H, 33, 39)(H, 35, 40)

SMILES Code: O=C(C1=CC(C2=CC(N3CCN(C)CC3)=NC=C2)=CC4=C1C=NN4C(C)C)NCC5=C(CCC)C=C(C)NC5=O