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GSK-503 was designed by performing high-throughput screening for EZH2 methyltransferase inhibiting compounds followed by chemical optimization.In a melanoma mouse model, conditional Ezh2 ablation as much as treatment with the preclinical EZH2 inhibitor GSK503 stabilizes the disease through inhibition of growth and virtually abolishes metastases formation without affecting normal melanocyte biology.GSK-503 inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency and is structurally related to GSK-126 and GSK-343. GSK-503 was > 200 fold selective over EZH1 (Kappi=636nM) and > 4000 fold selective over other histone methyltransferases.
| Molecular Weight | 526.67 |
| Formula | C31H38N6O2 |
| CAS Number | 1346572-63-1 |
| Solubility (25°C) | DMSO 44 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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