EPZ005687

EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2). It acts competitively with the EZH2 substrate S-adenosylmethionine. EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1. It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50 = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.Formal Name: 1-cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-1H-indazole-4-carboxamide. CAS Number: 1396772-26-1. Molecular Formula: C32H37N5O3. Formula Weight: 539.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 259, 312 nm. SMILES: O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C3=CC=C(CN4CCOCC4)C=C3)=CC5=C2C=NN5C6CCCC6. InChi Code: InChI=1S/C32H37N5O3/c1-21-15-22(2)35-32(39)28(21)18-33-31(38)27-16-25(17-30-29(27)19-34-37(30)26-5-3-4-6-26)24-9-7-23(8-10-24)20-36-11-13-40-14-12-36/h7-10,15-17,19,26H,3-6,11-14,18,20H2,1-2H3,(H,33,38)(H,35,39). InChi Key: ZOIBZSZLMJDVDQ-UHFFFAOYSA-N.