A-366

Catalog No.S7572

For research use only.

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

A-366 Chemical Structure

CAS No. 1527503-11-2

Selleck's A-366 has been cited by 4 Publications

Purity & Quality Control

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, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.
Targets
G9a/GLP [2]
(Cell-free assay)
3.3 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[1].

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].

Protocol (from reference)

Cell Research:[1]
  • 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.
Animal Research:[1]
  • Animal Models: SCID-beige female mice(AML flank xenograft model)
  • Dosages: 30 mg/kg/day
  • Administration: by osmotic mini-pump

Solubility (25°C)

In vitro

DMSO 65 mg/mL
(197.3 mM)
Ethanol 65 mg/mL
(197.3 mM)
Water Insoluble

Chemical Information

Molecular Weight 329.44
Formula

C19H27N3O2

CAS No. 1527503-11-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=C(C=C2C(=C1)C3(CCC3)C(=N2)N)OCCCN4CCCC4

In vivo Formulation Calculator (Clear solution)

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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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Molarity Calculator

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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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