UNC0224

The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development. UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM. Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).Formal Name: 7-[3-(dimethylamino)propoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine. CAS Number: 1197196-48-7. Molecular Formula: C26H43N7O2. Formula Weight: 485.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2.5 mg/ml, DMSO: 2 mg/ml, Ethanol: 15 mg/ml, PBS (pH 7.2): 2.5 mg/ml. lambdamax: 251, 346 nm. SMILES: COC1=CC2=C(NC3CCN(C)CC3)N=C(N4CCN(C)CCC4)N=C2C=C1OCCCN(C)C. InChi Code: InChI=1S/C26H43N7O2/c1-30(2)10-7-17-35-24-19-22-21(18-23(24)34-5)25(27-20-8-13-32(4)14-9-20)29-26(28-22)33-12-6-11-31(3)15-16-33/h18-20H,6-17H2,1-5H3,(H,27,28,29). InChi Key: XIVUGRBSBIXXJE-UHFFFAOYSA-N.