UNC0646

G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM). It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases. UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line. This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor.Formal Name: N-(1-cyclohexyl-4-piperidinyl)-2-[hexahydro-4-(1-methylethyl)-1H-1,4-diazepin-1-yl]-6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine. CAS Number: 1320288-17-2. Molecular Formula: C36H59N7O2. Formula Weight: 621.9. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 5 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 213, 250, 348 nm. SMILES: CC(C)N(CCC1)CCN1C2=NC(C=C(OCCCN3CCCCC3)C(OC)=C4)=C4C(NC(CC5)CCN5C6CCCCC6)=N2. InChi Code: InChI=1S/C36H59N7O2/c1-28(2)41-19-10-20-43(24-23-41)36-38-32-27-34(45-25-11-18-40-16-8-5-9-17-40)33(44-3)26-31(32)35(39-36)37-29-14-21-42(22-15-29)30-12-6-4-7-13-30/h26-30H,4-25H2,1-3H3,(H,37,38,39). InChi Key: OUKWLRHRXOPODD-UHFFFAOYSA-N.