Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC50: 18 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 40.00 | |
5 mg | In stock | $ 89.00 | |
10 mg | In stock | $ 132.00 | |
25 mg | In stock | $ 218.00 | |
50 mg | In stock | Inquiry | |
1 mL * 10 mM (in DMSO) | In stock | $ 95.00 |
Description | A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC50: 18 nM). |
Targets&IC50 | PRC2:18 nM |
In vitro | The embryonic ectoderm development (EED) protein is an essential subunit of PRC2. A-395 antagonizes the H3K27me3 binding functions of EED. A-395 binds to EED in the H3K27me3-binding pocket, thereby preventing allosteric activation of the catalytic activity of PRC2. A-395 is capable of competing for H3K27me3 peptide binding to EED (IC50: 7 nM). A-395, but not the close chemical analog A-395N, modulates the activity of PRC2 in cells by potently reducing the H3K27 methyl mark in a highly selective manner. A-395 treatment inhibits both H3K27me2 and H3K27me3 (IC50s: 390 nM and 90 nM). Furthermore, A-395 treatment results in growth inhibition of human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors. |
Cell Research | 1,000 multiple myeloma cells are seeded in each well of 96-well cell culture plates and treated with A-395 (0.001-100 μM) or DMSO control for 10 d before the cell proliferation assay. Cell proliferation assays are conducted with the CellTiter-Glo Luminescent Cell Viability Assay. |
Molecular Weight | 486.65 |
Formula | C26H35FN4O2S |
CAS No. | 2089148-72-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (205.49 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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A-395 2089148-72-9 Chromatin/Epigenetic Histone Methyltransferase A395 Inhibitor A 395 inhibit inhibitor