Description
GSK503 is a potent, specific EZH2 methyltransferase inhibitor that inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency (Ki app=3-27nM); GSK503 is highly selective for the SET domain of EZH2, >200 fold selective over EZH1 and >4000 fold selective over other HMTases; inhibits GCB lymphoma cell lines with IC50 of 0.5-20uM; impairs proliferation and invasiveness, accompanied by re-expression of tumour suppressor in melanoma cells; stabilizes the disease through inhibition of growth and virtually abolishes metastases formation without affecting normal melanocyte biology in melanoma mouse model