655203 Sigma-AldrichTX-1918 - CAS 503473-32-3 - Calbiochem
A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K, while it inhibits other kinases at much higher concentrations.
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Synonyms: 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
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Přehled
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Tabulka spec. kláve
| CAS # | Empirical Formula |
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| 503473-32-3 | C₁₄H₁₂O₃ |
Products
| Katalogové číslo | Balení | ks/bal. | |
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| 655203-10MG | Plastová ampulka | 10 mg |
| Description | |
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| Overview | A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC50 = 440 nM), while it inhibits other kinases at much higher concentrations (IC50 = 4.4, 44, 44, and 440 µM for Src, PKA, PKC, and EGFR-K, respectively). Displays potent antitumor activity (EC50 = 2.07 and 230 µM in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-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 | 655203 |
| Brand Family | Calbiochem® |
| Synonyms | 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione |
| References | |
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| References | Hori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257. |
| Product Information | |
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| CAS number | 503473-32-3 |
| ATP Competitive | N |
| Form | Light orange solid |
| Hill Formula | C₁₄H₁₂O₃ |
| Chemical formula | C₁₄H₁₂O₃ |
| Reversible | N |
| Structure formula Image | |
| Quality Level | MQ100 |
| Applications |
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| Biological Information | |
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| Primary Target | eEF2-K |
| Primary Target IC<sub>50</sub> | 440 nM against eEF2-K |
| Purity | ≥95% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
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| Safety Information according to GHS |
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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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| Katalogové číslo | GTIN |
| 655203-10MG | 04055977184716 |
Documentation
TX-1918 - CAS 503473-32-3 - Calbiochem MSDS
| Title |
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TX-1918 - CAS 503473-32-3 - Calbiochem Certificates of Analysis
| Title | Lot Number |
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| 655203 |
References
| Přehled odkazů |
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| Hori, H., et al. 2002. Bioorg. Med. Chem. 10, 3257. |