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GSK126
Description
GSK126 is a highly effective, highly selective, S-adenosyl-methionine competitive small molecule inhibitor of EZH2 methyltransferase activity that reduces global H3K27me3 levels and reactivates silenced PRC2 target genes.
Basic Information
Synonyms: | GSK 126; GSK-126 |
Application: | EZH2 Inhibitor |
CAS Number: | 1346574-57-9 |
Formula: | C31H38N6O2 |
Molecular Weight: | 526.67 |
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 |
Solubility-In vitro: | In vitro (25°C): DMSO: Warmed: 3 mg/mL (5.69 mM) Water: Insoluble Ethanol: Insoluble |
Solubility-In vivo: | 4% DMSO+corn oil: 0.4 mg/mL |
Target Info
EZH2: | 9.9 nM |
Storage
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Preparing Stock Solutions
0.1 mM_1 mg: 18.99 mL
0.1 mM_5 mg: 94.94 mL
0.1 mM_10 mg: 189.87 mL
0.5 mM_1 mg: 3.8 mL
0.5 mM_5 mg: 18.99 mL
0.5 mM_10 mg: 37.97 mL
1 mM_1 mg: 1.9 mL
1 mM_5 mg: 9.49 mL
1 mM_10 mg: 18.99 mL
5 mM_1 mg: 0.38 mL
5 mM_5 mg: 1.9 mL
5 mM_10 mg: 3.8 mL
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