655200 Sigma-AldrichTX-1123 - CAS 157397-06-3 - Calbiochem
A cell-permeable, reversible, and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as an inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC at much higher concentrations.
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同义词: 2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione, PKA Inhibitor XII
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概述
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重要规格表
| CAS # | Empirical Formula |
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| 157397-06-3 | C₂₀H₂₄O₃ |
Products
| 产品目录编号 | 包装 | 数量 / 包装 | |
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| 655200-10MGCN | 塑胶安瓿;塑胶针药瓶 | 10 mg |
| Description | |
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| Overview | A cell-permeable, reversible, and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as an inhibitor for Src, eEF2-K, and PKA (IC50 = 2.2, 3.2, and 9.6 µM, respectively), while it inhibits EGFR-K and PKC at much higher concentrations (IC50 = 320 µM). Displays potent antitumor activity (EC50 = 3.66 and 39 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥1000-fold) and hepato-toxicity (≥50-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). It is therefore a more promising candidate as a therapeutic agent for cancer treatment. |
| Catalogue Number | 655200 |
| Brand Family | Calbiochem® |
| Synonyms | 2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione, PKA Inhibitor XII |
| References | |
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| References | Hori, H., et al. 2003. Cell. Mol. Biol. Lett. 8, 528. Hori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257. |
| Product Information | |
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| CAS number | 157397-06-3 |
| ATP Competitive | Y |
| Form | Yellow solid |
| Hill Formula | C₂₀H₂₄O₃ |
| Chemical formula | C₂₀H₂₄O₃ |
| Reversible | Y |
| Structure formula Image | |
| Quality Level | MQ100 |
| Applications |
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| Biological Information | |
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| Primary Target | Src |
| Primary Target IC<sub>50</sub> | 2.2, 3.2, and 9.6 µM against Src, eEF2-K, and PKA, respectively |
| Purity | ≥95% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
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| Materials Information |
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| Toxicological Information |
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| Safety Information according to GHS |
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| Safety Information |
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| Product Usage Statements |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| 产品目录编号 | GTIN |
| 655200-10MGCN | 04055977184709 |
Documentation
TX-1123 - CAS 157397-06-3 - Calbiochem MSDS
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TX-1123 - CAS 157397-06-3 - Calbiochem 分析证书
| 标题 | 批号 |
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| 655200 |
参考
| 参考信息概述 |
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| Hori, H., et al. 2003. Cell. Mol. Biol. Lett. 8, 528. Hori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257. |