A-366

A-366 is a potent, peptide-competitive inhibitor of the lysine methyltransferase G9a (IC50 = 3.3 nM). It displays greater than 1,000-fold selectivity over 21 other methyltransferases. A-366 significantly reduces the cellular levels of dimethylation on histone 3 at lysine 9 (H3K9Me2) in PC3 cells without reducing total histone 3, H3K27Me3, or H3K36Me2. It also blocks the interaction of the methyl lysine reader protein Spindlin1 with H3K4me3 by binding with a Spindlin1 Tudor domain (Kd = 111 nM). See the Structural Genomics Consortium (SGC) website for more information.Formal Name: 5'-methoxy-6'-[3-(1-pyrrolidinyl)propoxy]-spiro[cyclobutane-1,3'-[3H]indol]-2'-amine. CAS Number: 1527503-11-2. Molecular Formula: C19H27N3O2. Formula Weight: 329.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 222, 283 nm. SMILES: NC1=NC2=CC(OCCCN3CCCC3)=C(OC)C=C2C14CCC4. InChi Code: InChI=1S/C19H27N3O2/c1-23-16-12-14-15(21-18(20)19(14)6-4-7-19)13-17(16)24-11-5-10-22-8-2-3-9-22/h12-13H,2-11H2,1H3,(H2,20,21). InChi Key: BKCDJTRMYWSXMC-UHFFFAOYSA-N.