Welcome to GenPrice! Check out our latest updates.

Shopping Cart (0)

Your cart is empty

Add some products to get started!

A-366

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].

Product Specifications

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)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-12583/A-366-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-12583/A-366-SDS-MedChemExpress.pdf

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

EHMT1/GLP/KMT1D; EHMT2/G9a/KMT1C

Available Sizes

Curated Selection

Explore Other Products

Discover premium biology products from our extensive collection of 20M+ items

NSA2 AAV Vector (Mouse) (CMV)
32189104 1 μg

NSA2 AAV Vector (Mouse) (CMV)

Ask
View Details
Exocyst Complex Component 3 Rabbit Monoclonal Antibody
E10G21966 100 µL

Exocyst Complex Component 3 Rabbit Monoclonal Antibody

Ask
View Details
Gtf2h2 (BC016231) Mouse Tagged Lenti ORF Clone
MR206255L4 10 µg

Gtf2h2 (BC016231) Mouse Tagged Lenti ORF Clone

Ask
View Details
Lentiviral human CHEK1 sgRNA gene knockout kit - Lentiviral human CHEK1 sgRNA gene knockout kit (25)
GTR15398163 1 Vial

Lentiviral human CHEK1 sgRNA gene knockout kit - Lentiviral human CHEK1 sgRNA gene knockout kit (25)

Ask
View Details