Name: A-366
Brand: Selleck Chemicals
SKU: S7572
Rating: 5 (8 reviews)

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

CAS: 1527503-11-2

Selleck's A-366 has been cited by 8 publications

Purity & Quality Control

Batch: Purity: 99.23%

99.23

A-366 Related Products

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Signaling Pathway

Histone Methyltransferase Signaling Pathway

Choose Selective Histone Methyltransferase Inhibitors

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

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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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

Tel: +1-832-582-8158 Ext:3
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