EI1

The lysine methyltransferase EZH2 (KMT6), part of polycomb repressive complex 2 (PRC2), catalyzes trimethylation of lysine 27 on histone H3 (H3K27) and is involved in proliferation and aggressive cell growth associated with neoplastic cells. EI1 is an EZH2 inhibitor that has activity against both wild-type and Y641F mutant EZH2 (IC50s = 15 and 13 nM, respectively). It displays 90-fold selectivity for EZH2 over EZH1 and >10,000-fold over other lysine methyltransferases. EI1 blocks cellular H3K27 methylation and activates PRC2-specific gene expression. Inhibition of EZH2 by EI1 in diffused large B cell lymphoma cells carrying Y641 mutations results in decreased proliferation, cell cycle arrest, and apoptosis.Formal Name: 6-cyano-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-ethylpropyl)-1H-indole-4-carboxamide. CAS Number: 1418308-27-6. Molecular Formula: C23H26N4O2. Formula Weight: 390.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 2 mg/ml. lambdamax: 250, 309 nm. SMILES: O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C#N)=CC3=C2C=CN3C(CC)CC. InChi Code: InChI=1S/C23H26N4O2/c1-5-17(6-2)27-8-7-18-19(10-16(12-24)11-21(18)27)22(28)25-13-20-14(3)9-15(4)26-23(20)29/h7-11,17H,5-6,13H2,1-4H3,(H,25,28)(H,26,29). InChi Key: PFHDWRIVDDIFRP-UHFFFAOYSA-N.