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A-395
Catalog No. T10205Cas No. 2089148-72-9
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).
A-395
Catalog No. T10205Cas No. 2089148-72-9
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 |
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Purity:97.82%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 |
Storage & Solubility Information
| 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 | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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