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Formula | C19H27N3O2 |
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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 | |||
* <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.) |
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. | ||||
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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]. |
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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]. |
Cell Assay: |
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Animal Study: |
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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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.