A-366

Catalog No.S7572 Batch:S757202

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Technical Data

Formula

C19H27N3O2
Molecular Weight 329.44 CAS No. 1527503-11-2
Solubility (25°C)* In vitro DMSO 65 mg/mL (197.3 mM)
Ethanol 65 mg/mL (197.3 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5% DMSO 95% Corn oil
3.25mg/ml
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.25mg/ml
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 Assay:

[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 Study:

[1]
  • Animal Models

    SCID-beige female mice(AML flank xenograft model)

  • Dosages

    30 mg/kg/day

  • Administration

    by osmotic mini-pump

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

Chronic hypoxia stabilizes 3βHSD1 via autophagy suppression [ Cell Rep, 2024, 43(1):113575] PubMed: 38181788
Inhibition of EHMT1/2 rescues synaptic damage and motor impairment in a PD mouse model [ Cell Mol Life Sci, 2024, 81(1):128] PubMed: 38472451
Euchromatic Histone Lysine Methyltransferase 2 Inhibition Enhances Carfilzomib Sensitivity and Overcomes Drug Resistance in Multiple Myeloma Cell Lines [ Cancers (Basel), 2023, 15(8)2199] PubMed: 37190128
Inhibition of the CtBP complex and FBXO11 enhances MHC class II expression and anti-cancer immune responses [ Cancer Cell, 2022, 40(10):1190-1206.e9] PubMed: 36179686
BRD4770 functions as a novel ferroptosis inhibitor to protect against aortic dissection [ Pharmacol Res, 2022, 177:106122] PubMed: 35149187
Inhibition of a G9a/DNMT network triggers immune-mediated bladder cancer regression. [ Nat Med, 2019, 25(7):1073-1081] PubMed: 31270502
Dynamic reversal of random X-Chromosome inactivation during iPSC reprogramming. [ Genome Res, 2019, 29(10):1659-1672] PubMed: 31515287
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] PubMed: 30135193

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.