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GSK503 is a specific EZH2 methyltransferase inhibitor or vehicle. GSK503 was designed by performing high-throughput screening for EZH2 methyltransferase inhibiting compounds followed by chemical optimization.GSK503 inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency (Kappi=3−27nM) and is structurally related to GSK126 and GSK343. GSK503 was > 200 fold selective over EZH1 (Kappi=636nM) and > 4000 fold selective over other histone methyltransferases. GSK503 displayed favorable pharmacokinetics in mice and was thus selected for use in in vivo experiments. For the detailed information of GSK-503, the solubility of GSK-503 in water, the solubility of GSK-503 in DMSO, the solubility of GSK-503 in PBS buffer, the animal experiment (test) of GSK-503, the cell expriment (test) of GSK-503, the in vivo, in vitro and clinical trial test of GSK-503, the EC50, IC50,and affinity,of GSK-503, For the detailed information of GSK-503, the solubility of GSK-503 in water, the solubility of GSK-503 in DMSO, the solubility of GSK-503 in PBS buffer, the animal experiment (test) of GSK-503, the cell expriment (test) of GSK-503, the in vivo, in vitro and clinical trial test of GSK-503, the EC50, IC50,and affinity,of GSK-503, Please contact DC Chemicals. |