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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 | Price | Availability | Quantity |
---|---|---|---|
1 mg | $40 | In Stock | |
5 mg | $89 | In Stock | |
10 mg | $132 | In Stock | |
25 mg | $218 | In Stock | |
50 mg | Inquiry | In Stock | |
1 mL x 10 mM (in DMSO) | $95 | In Stock |
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 by binding to the H3K27me3-binding pocket, thereby preventing the allosteric activation of PRC2's catalytic activity. A-395 competes for H3K27me3 peptide binding to EED (IC50: 7 nM) and selectively modulates PRC2 activity in cells, markedly reducing the H3K27 methyl mark. A-395 inhibits H3K27me2 and H3K27me3 (IC50s: 390 nM and 90 nM, respectively) and induces growth inhibition in human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors, unlike its close chemical analog A-395N. |
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 |
Smiles | CN(C)[C@H]1CN(C[C@@H]1c1ccc(cc1)N1CCN(CC1)S(C)(=O)=O)C1CCc2cccc(F)c12 |
Relative Density. | 1.30 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (205.49 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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