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A-366

Catalog No. T3624 CAS 1527503-11-2

Synonyms: A 366, A366

A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families.

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A-366, CAS 1527503-11-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 43.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 92.00
25 mg	In stock	$ 219.00
50 mg	In stock	$ 378.00
100 mg	In stock	$ 558.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Purity: 99.8%

Purity: 98.53%

Purity: 97.28%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families.
Targets&IC50	G9a/GLP:3.3 nM
Kinase Assay	7.5× compounds are added to a 96-well PolyPlate containing 60 μL of Buffer per well with substrates CoA (200 μM), ATP (400 μM), and [14C]citrate. Reaction is started with 4 μL (300 ng/well) ACL, and the plate is incubated at 37°C for 3 h. Th
Cell Research	PC-3 prostate adenocarcinoma cells are incubated in triplicate with DMSO or the indicated concentrations of A-366 or UNC0638 for 72 hours. H3K9me2 levels are assessed by In-Cell Western assay. (Only for Reference)

Synonyms	A 366, A366
Molecular Weight	329.44
Formula	C19H27N3O2
CAS No.	1527503-11-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

1eq. HCl: 32.9 mg/mL (100 mM)

DMSO: 32.9 mg/mL (100 mM)

References and Literature

1. Pappano WN, et al. PLoS One. 2015, 10(7):e0131716. 2. Sweis RF, et al. ACS Med Chem Lett. 2014, 5(2):205-209. 3. Zhang W, Yang D, Yuan Y, et al. Muscular G9a regulates muscle-liver-fat axis by musclin under overnutrition in female mice[J]. Diabetes. 2020

Citations

1. Zhang W, Yang D, Yuan Y, et al. Muscular G9a regulates muscle-liver-fat axis by musclin under overnutrition in female mice. Diabetes. 2020 2. Yang D, Fan Y, Xiong M, et al.Loss of renal tubular G9a benefits acute kidney injury by lowering focal lipid accumulation via CES1.EMBO reports.2023: e56128.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Target-Focused Phenotypic Screening Library PPI Inhibitor Library Methylation Compound Library Chromatin Modification Compound Library Bioactive Compounds Library Max Epigenetics Compound Library Stem Cell Differentiation Compound Library NO PAINS Compound Library

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Keywords

A-366 1527503-11-2 Chromatin/Epigenetic Epigenetic Reader Domain Histone Methyltransferase epigenetics interaction A 366 H3K4me3 A366 inhibit selective peptide-competitive Inhibitor methyltransferase cells inhibitor

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