Home Epigenetics Histone Methyltransferase inhibitor - G9a/GLP inhibitor A-366 For research use only.

A-366

A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM and 38nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.

A-366 Chemical Structure

A-366 Chemical Structure

CAS No. 1527503-11-2

Purity & Quality Control

A-366 Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Biological Activity

Description A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM and 38nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.
Targets
G9a [2]
(Cell-free assay)		 GLP [2]
3.3 nM 38 nM
In vitro
In vitro

A-366 has significantly less cytotoxic effects on the growth of tumor cell lines compared to other known G9a/GLP small molecule inhibitors despite equivalent cellular activity on methylation of H3K9me2. Treatment of various leukemia cell lines in vitro results in marked differentiation and morphological changes of these tumor cell lines[1].
Cell Research Cell lines PC-3 prostate adenocarcinoma cells
Concentrations 0, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
Incubation Time 72 h
Method

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.
In Vivo
In vivo

Treatment of a flank xenograft leukemia model with A-366 results in growth inhibition consistent with the profile of H3K9me2 reduction observed[1].
Animal Research Animal Models SCID-beige female mice(AML flank xenograft model)
Dosages 30 mg/kg/day
Administration by osmotic mini-pump

Chemical Information & Solubility

Molecular Weight 329.44 Formula

C19H27N3O2
CAS No. 1527503-11-2 SDF Download A-366 SDF
Smiles COC1=C(C=C2C(=C1)C3(CCC3)C(=N2)N)OCCCN4CCCC4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 65 mg/mL ( (197.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 65 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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