EPZ020411

EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6, IC50 = 10 nM) that less potently targets PRMT1 and PRMT8 (IC50s = 119 and 223 nM, respectively). It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC50 = 0.637 µM). EPZ020411 shows a moderate clearance rate in rats following intravenous bolus administration, and, following 5 mg/kg subcutaneous dosing, has an unbound blood concentration exceeding the PRMT6 biochemical IC50 value for more than 12 hours.Formal Name: N1,N2-dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine. CAS Number: 1700663-41-7. Molecular Formula: C25H38N4O3. Formula Weight: 442.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 5 mg/ml, Ethanol: 1 mg/ml, PBS (pH 7.2): 0.3 mg/ml. lambdamax: 250 nm. SMILES: CN(CCNC)CC1=CNN=C1C(C=C2)=CC=C2O[C@H](C3)C[C@@H]3OCCC4CCOCC4. InChi Code: InChI=1S/C25H38N4O3/c1-26-10-11-29(2)18-21-17-27-28-25(21)20-3-5-22(6-4-20)32-24-15-23(16-24)31-14-9-19-7-12-30-13-8-19/h3-6,17,19,23-24,26H,7-16,18H2,1-2H3,(H,27,28)/t23-,24-. InChi Key: QMDKVNSQXPVCRD-RQNOJGIXSA-N.