For research use only. Not for therapeutic Use.
GSK126（Cat No.:I001332）is a selective small molecule inhibitor of the enhancer of zeste homolog 2 (EZH2), a key enzyme involved in the regulation of gene expression through histone modification. EZH2 is part of the polycomb repressive complex 2 (PRC2), which plays a critical role in maintaining cellular identity and silencing tumor suppressor genes. By inhibiting EZH2, GSK126 reactivates silenced genes and has shown potential in treating cancers, especially those with mutations or overexpression of EZH2, such as certain lymphomas and solid tumors. GSK126 is being studied in preclinical and clinical trials for its anticancer efficacy.
| Catalog Number | I001332 |
| CAS Number | 1346574-57-9 |
| Synonyms | 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide |
| Molecular Formula | C₃₁H₃₈N₆O₂ |
| Purity | ≥95% |
| Target | Histone Methyltransferase |
| Solubility | 50 mM in DMSO |
| Storage | Store at -20°C |
| IC50 | 0.5 nM (Ki) |
| IUPAC Name | 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide |
| 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 |
| SMILES | CC[C@H](C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C |
| Reference | 1:Blocking EZH2 methylation transferase activity by GSK126 decreases stem cell-like myeloma cells. Zeng D, Liu M, Pan J.Oncotarget. 2017 Jan 10;8(2):3396-3411. doi: 10.18632/oncotarget.13773. PMID: 27926488 Free PMC Article<br /> |
