1527503-11-2
Chemical Structure
A-366
- CAS No.: 1527503-11-2
- Formula:C19H27N3O2
- Molecular Weight:329.44
IUPAC Name: 5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine
InChIKey: BKCDJTRMYWSXMC-UHFFFAOYSA-N
SMILES: COC1=CC2=C(N=C(N)C23CCC3)C=C1OCCCN4CCCC4
Biological Activity: A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families[1][2][3][4].
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A-366 | 98.84% | A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families. | ||||||||||||||||||||
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References
- [1]. Reiner D, et al. Epigenetics meets GPCR: inhibition of histone H3 methyltransferase (G9a) and histamine H3 receptor for Prader-Willi Syndrome. Sci Rep. 2020;10(1):13558. Published 2020 Aug 11. [Content Brief]
- [2]. Wagner T, et al. Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform. Nucleic Acids Res. 2016;44(9):e88. [Content Brief]
- [3]. Sweis RF, et al. Discovery and development of potent and selective inhibitors of histone methyltransferase g9a. ACS Med Chem Lett. 2014;5(2):205-209. Published 2014 Jan 2. [Content Brief]
- [4]. Pappano WN, et al. The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia. PLoS One. 2015;10(7):e0131716. Published 2015 Jul 6. [Content Brief]
