WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407285
Description: A-366 is a potent inhibitor of G9a/GLP with IC50 3 nM and > 100-fold selectivity over other methyltransferases and other non-epigenetic targets. A-366 has been shown to inhibit H3K9 methylation in cells with an IC50 of 100 nM and exhibits minimal cellular toxicity compared with previous quinazoline-based probes. A-366 selectively inhibits G9a and the closely related GLP (EHMT1), but not other histone methyltransferases. A-366 has significantly less cytotoxic effects on the growth of tumor cell lines compared to other known G9a/GLP small molecule inhibitors despite equivalent cellular activity on methylation of H3K9me2.
MedKoo Cat#: 407285
Chemical Formula: C19H27N3O2
Exact Mass: 329.2103
Molecular Weight: 329.444
Elemental Analysis: C, 69.27; H, 8.26; N, 12.76; O, 9.71
Synonym: A-366; A 366; A366.
IUPAC/Chemical Name: 5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine
InChi Key: BKCDJTRMYWSXMC-UHFFFAOYSA-N
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)
SMILES Code: NC(C12CCC1)=NC3=C2C=C(OC)C(OCCCN4CCCC4)=C3
1: 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. The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for
G9a/GLP in the Epigenetics of Leukemia. PLoS One. 2015 Jul 6;10(7):e0131716. doi:
10.1371/journal.pone.0131716. eCollection 2015. PubMed PMID: 26147105; PubMed
Central PMCID: PMC4492996.