A-366

• Description :

  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].

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  Epigenetic Reader Domain; Histone Methyltransferase

• Type :

  Reference compound

• Related Pathways :

  Epigenetics

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/A-366.html

• Purity :

  98.01

• Solubility :

  DMSO : 50 mg/mL (ultrasonic)

• Smiles :

  COC1=CC2=C(N=C(N)C23CCC3)C=C1OCCCN4CCCC4

• Molecular Formula :

  C19H27N3O2

• Molecular Weight :

  329.44

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [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.|[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.|[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.|[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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  EHMT1/GLP/KMT1D; EHMT2/G9a/KMT1C

• CAS Number :

  [1527503-11-2]