Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
説明 | 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. |
ターゲット&IC50 | G9a/GLP:3.3 nM |
キナーゼ試験 | 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 |
細胞研究 | 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) |
別名 | A 366, A366 |
分子量 | 329.44 |
分子式 | C19H27N3O2 |
CAS No. | 1527503-11-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
1eq. HCl: 32.9 mg/mL (100 mM)
DMSO: 32.9 mg/mL (100 mM)
You can also refer to dose conversion for different animals. 詳細
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A-366 1527503-11-2 Chromatin/Epigenetic Epigenetic Reader Domain Histone Methyltransferase epigenetics interaction A 366 H3K4me3 A366 inhibit selective peptide-competitive Inhibitor methyltransferase cells inhibitor