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GSK 126
- GSK2816126
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C31H38N6O2
- MW: 526.67
Description
GSK 126 (GSK2816126) is a potent, selective and cell-active EZH2 histone lysine methyltransferase inhibitor with reported Ki of 0.57 nM and IC50 of 9.9 nM. It is more than 150-fold selective for EZH2 over EZH1 and has been profiled against other human methyltransferases.
EZH2 is the catalytic PRC2 subunit responsible for H3K27 methylation and is frequently dysregulated in lymphoma and solid tumors. GSK 126 is relevant for epigenetic oncology studies and EZH2-mutant DLBCL models.
Key Features
- Potent EZH2 histone methyltransferase inhibitor
- Cell-active inhibitor of H3K27 methylation
- Selective over EZH1 and other methyltransferases
- Inhibits EZH2-mutant DLBCL cell and xenograft growth
Applications
- EZH2 enzymatic assays
- H3K27 methylation studies
- Epigenetic oncology research
- DLBCL and PRC2 pathway models
More Information
| 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 |
References
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