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A-366
$40 – $460
Products Details
Product Description
– A-366 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].
Web ID
– HY-12583
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C19H27N3O2
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.|[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.
CAS Number
– 1527503-11-2
Molecular Weight
– 329.44
Compound Purity
– 98.02
SMILES
– COC1=CC2=C(N=C(N)C23CCC3)C=C1OCCCN4CCCC4
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– DMSO : 50 mg/mL (ultrasonic)
Target
– Epigenetic Reader Domain;Histone Methyltransferase
Isoform
– EHMT1/GLP/KMT1D;EHMT2/G9a/KMT1C
Pathway
– Epigenetics
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
