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您的位置:首頁>>分析化學>>藥物分析標準品>>G7340 GSK-126 1346574-57-9
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.


References

Tian 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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