A-366

Catalog No.S7572

A-366 Chemical Structure

Molecular Weight(MW): 329.44

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.

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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

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: SCID-beige female mice(AML flank xenograft model)
  • Formulation: 98% PEG-400 and 2% Tween-80
  • Dosages: 30 mg/kg/day
  • Administration: by osmotic mini-pump
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 329.44
Formula

C19H27N3O2

CAS No. 1527503-11-2
Storage powder
Synonyms N/A

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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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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID