| 产品详情 |
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| Product Name | ATR Inhibitor IV |
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| Description | Purity ~90% (HPLC). A cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive (Ki= 13nM; IC50/[ATP] = 70nM/50uM and 128nM/100uM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs (Ki= 2.2, 3.9, 16, and >1uM, respectively, against DNA-PK, PI 3-K-gamma, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 & Chk1 Ser345 phosphorylation (complete inhibition at 10uM in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24h) VE-821 treatment, either alone or in synergy with Cisplatin, results in reversible cytostatic growth arrest regardless of cellular ATM-p53 pathway activity, while cytotoxicity and Cisplatin synergism in cell death induction is reported to occur only upon long-term VE-821 exposure (≥72h) in cultures with ATM-p53 pathway defects. Solubility: As reported Primary Target: ATR Primary Target Ki: 13nM Molar Mass |
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| Size | 10mg |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | ATR Inhibitor IV (VE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV) |
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| Gene, Accession, CAS # | n/a |
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| Catalog # | 217200 |
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| Order / More Info | ATR Inhibitor IV from UNITED STATES BIOLOGICAL |
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| Product Specific References | n/a |
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