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A-366 Histone Methyltransferase inhibitor

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

Cat.No.S7572

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.

Chemical Structure

Molecular Weight: 329.44

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Quality Control

Batch: Purity: 99.23%

99.23

Related Targets	HDAC JAK BET PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other Histone Methyltransferase Inhibitors	Pinometostat (EPZ5676) 3-Deazaneplanocin A (DZNep) Hydrochloride BIX-01294 trihydrochloride EPZ004777 EPZ015666 (GSK3235025) UNC1999 EPZ005687 SGC 0946 MM-102 UNC0638

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (197.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 65 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.250mg/ml (9.87mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.250mg/ml (9.87mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	329.44	Formula	C₁₉H₂₇N₃O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1527503-11-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=C(C=C2C(=C1)C3(CCC3)C(=N2)N)OCCCN4CCCC4

Mechanism of Action

Targets/IC₅₀/Ki	G9a (Cell-free assay) 3.3 nM GLP 38 nM
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.
In vivo	Treatment of a flank xenograft leukemia model with A-366 results in growth inhibition consistent with the profile of H3K9me2 reduction observed.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26147105/ [2] https://pubmed.ncbi.nlm.nih.gov/24900801/

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