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| Cat. Number | G7340 |
| Chemical Name | G7340 GSK-126 1346574-57-9 |
| CAS Number | 1346574-57-9 |
| Mol. Formula | C31H38N6O2 |
| Mol. Weight | 526.67 |
| Qty 1 |
1mg |
| Qty 2 | 25mg |
| Appearance | tan powder |
| Application Notes | ≥98%, ≥99%ee |
| Synonym | GSK126 |
| Solubility | DMSO 3 mg/mL warmed (5.69 mM) Water Insoluble Ethanol Insoluble warmed |
| Storage condition | -20°C |
| References | GSK-126 is an inhibitor of mutant EZH2, a histone methyltransferase (HMT) that exhibits point mutations at key residues Tyr641 and Ala677; this compound does not appreciably affect WT EZH2. EZH2 is responsible for modulating expression of a variety of genes. GSK-126 competes with cofactor S-adenylmethionine (SAM) for binding to EZH2. GSK-126 displays anticancer chemotherapeutic activity by inhibiting proliferation in in vitro and in vivo models of diffuse large B-cell lymphoma. ReferencesTian X, Zhang S, Liu HM, et al. Histone lysine-specific methyltransferases and demethylases in carcinogenesis: new targets for cancer therapy and prevention. Curr Cancer Drug Targets. 2013 Jun 10;13(5):558-79. PMID: 23713993. McCabe MT, Ott HM, Ganji G, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012 Dec 6;492(7427):108-12. PMID: 23051747. |
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