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GSK 126

Axon 2140
CAS:  1346574-57-9
  • Optical Purity:  Optically pure
  • Soluble in DMSO
  • MF:  C31H38N6O2
  • MW:  526.67

Description

Potent, selective, cell-active inhibitor of histone lysine methyltransferase (HMTase or HMT; H3K27 selective) EZH2 (Ki 0.57 nM; IC50 9.9 nM); more than 150-fold selective for EZH2 versus EZH1 (Ki 89 nM) and 20 other human methyltransferases. GSK126 effectively inhibits proliferation of EZH2 mutant DLBCL cell lines and growth of EZH2 mutant DLBCL xenografts in mice.

More Information

Certificate of Analysis

Material Safety Data Sheet

Parent CAS No. 1346574-57-9
Chemical Name (S)-1-sec-butyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
SMILES N1([C@@H](C)CC)C2=C(C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C3=CC=C(N4CCNCC4)N=C3)=C2)C(C)=C1 |&1:1,r|
MFCD N.A.
InChi InChI=1S/C31H38N6O2/c1-6-22(5)37-18-20(3)29-25(30(38)34-17-26-19(2)13-21(4)35-31(26)39)14-24(15-27(29)37)23-7-8-28(33-16-23)36-11-9-32-10-12-36/h7-8,13-16,18,22,32H,6,9-12,17H2,1-5H3,(H,34,38)(H,35,39)/t22-/m0/s1
InChiKey FKSFKBQGSFSOSM-QFIPXVFZSA-N
CID 68210102
Short Description EZH2 HMTase inhibitor

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