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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 |
| Related Histone Methyltransferase Products |
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| EPZ-5676
EPZ-5676 is a potent and selective aminonucleoside inhibitor of DOT1L histone methyltransferase. |
| EPZ004777
EPZ004777 is a potent, selective, small-molecule inhibitor of DOT1L with IC50 of 0.4 nM. |
| 3-Deazaneplanocin A
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| EPZ004777 hydrochloride
EPZ004777 hydrochloride is the hydrochloride salt of EPZ004777, which is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM. |
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