A-366

CAT: 0804-HY-12583-01Size: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-12583-01Size:1 mg
Selected
AVAILABILITY: InStock
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
Product image 1
1 / 1
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].
CAS Number
[1527503-11-2]
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

Popular Products