A-366 NEW
Price | $30 | $43 | $68 |
Package | 1mg | 2mg | 5mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-18 |
Product Details
Product Name: A-366 | CAS No.: 1527503-11-2 |
Purity: 99.8% | Supply Ability: 10g |
Release date: 2024/11/18 |
Product Introduction
Bioactivity
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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | 1eq. HCl : 32.9 mg/mL (100 mM) DMSO : 32.9 mg/mL (100 mM) |
Keywords | epigenetics | interaction | H3K4me3 | A-366 | inhibit | Epigenetic Reader Domain | selective | peptide-competitive | Inhibitor | methyltransferase | cells |
Inhibitors Related | ABBV-744 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | Tazemetostat | Piribedil | GSK126 | Curcumin | EPZ015666 | dBET6 | Naphthol AS-E | MRTX-1719 | Bisdemethoxycurcumin |
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Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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