A-366

• CAT Number: I001902
• CAS Number: 1527503-11-2
• Molecular Formula: C₁₉H₂₇N₃O₂
• Molecular Weight: 329.44
• Purity: ≥95%
• Target: Histone Methyltransferase
• Solubility: 100 mM in DMSO
• Storage: Store at -20°C
• IC50: 3 nM
• InChI: 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)
• InChIKey: BKCDJTRMYWSXMC-UHFFFAOYSA-N
• SMILES: NC(C12CCC1)=NC3=C2C=C(OC)C(OCCCN4CCCC4)=C3

A-366(CAT: I001902) is a potent and selective peptide-competitive inhibitor of G9a/GLP. It displays an enzymatic IC50 of approximately 3 nM, demonstrating exceptional affinity for its target. This compound exhibits remarkable selectivity, with over 100-fold specificity towards G9a/GLP compared to other methyltransferases and non-epigenetic targets. By interfering with G9a/GLP activity, A-366 may play a crucial role in modulating epigenetic processes, potentially leading to valuable insights and therapeutic strategies related to epigenetic regulation.

Reference

1:The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia. Pappano WN, Guo J, He Y, Ferguson D, Jagadeeswaran S, Osterling DJ, Gao W, Spence JK, Pliushchev M, Sweis RF, Buchanan FG, Michaelides MR, Shoemaker AR, Tse C, Chiang GG.PLoS One. 2015 Jul 6;10(7):e0131716. doi: 10.1371/journal.pone.0131716. eCollection 2015. PMID: 26147105 Free PMC Article2:[Rheumatic disorders observed in HIV infected patients undergoing highly active antiretroviral therapy (HAART): a 366 case prospective study in Burkina Faso]. Ouédraogo DD, Lompo CP, Tiéno H, Bognounou R, Diendéré AE, Sawadogo A, Zoungrana L, Drabo JY.Med Trop (Mars). 2010 Aug;70(4):345-8. French. PMID: 22368930 3:Ultraviolet radiation-A (366 nm) induced morphological and histological malformations during embryogenesis of Clarias gariepinus (Burchell, 1822). Mahmoud UM, Mekkawy IA, Sayed Ael-D.J Photochem Photobiol B. 2009 May 4;95(2):117-28. doi: 10.1016/j.jphotobiol.2009.02.003. Epub 2009 Feb 20. PMID: 19285878 4:Analyses of truncated fibrillin caused by a 366 bp deletion in the FBN1 gene resulting in Marfan syndrome. Raghunath M, Kielty CM, Kainulainen K, Child A, Peltonen L, Steinmann B.Biochem J. 1994 Sep 15;302 ( Pt 3):889-96. PMID: 7945217 Free PMC Article5:[Reactions of various neuroregulatory systems in astronauts after a 366-day space flight]. Davydova NA.Fiziol Cheloveka. 1992 Jul-Aug;18(4):30-8. Russian. No abstract available. PMID: 1358735