| Name | A-366 |
| Description | A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families. |
| Cell Research | 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) |
| Kinase Assay | 7.5× compounds are added to a 96-well PolyPlate containing 60 μL of Buffer per well with substrates CoA (200 μM), ATP (400 μM), and [14C]citrate. Reaction is started with 4 μL (300 ng/well) ACL, and the plate is incubated at 37°C for 3 h. Th |
| In vitro | For tumor cell growth, A-366 had less toxic effects than some other G9a/GLP small molecule compound inhibitors, and no difference in the methylation effect on H3K9me2. Various leukemia cell lines were treated with A-366 in vitro, and these tumor cells would produce significant differentiation and morphological changes. |
| In vivo | For tumor cell growth, A-366 had less toxic effects than some other G9a/GLP small molecule compound inhibitors, and no difference in the methylation effect on H3K9me2. Various leukemia cell lines were treated with A-366 in vitro, and these tumor cells would produce significant differentiation and morphological changes. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.07 mM), Sonication is recommended.
DMSO : 32.9 mg/mL (99.87 mM), Sonication is recommended.
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| Keywords | selective | peptide-competitive | methyltransferase | interaction | Inhibitor | inhibit | HistoneMethyltransferase | Histone Methyltransferase | H3K4me3 | G9a/GLP | epigenetics | EpigeneticReaderDomain | Epigenetic Reader Domain | cells | A-366 |
| Inhibitors Related | MAK-683 hydrochloride | ABBV-744 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | Tazemetostat | Piribedil | 5-Ph-IAA | Curcumin | EPZ015666 | Naphthol AS-E | MRTX-1719 | JQ-1 (carboxylic acid) |
| Related Compound Libraries | Highly Selective Inhibitor Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Epigenetics Compound Library | Chromatin Modification Compound Library | Inhibitor Library | NO PAINS Compound Library | Stem Cell Differentiation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
