Erbstatin Analog (CAS 63177-57-1)
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Erbstatin Analog, also known as methyl 2,5-dihydroxycinnamate, is a stable analog of erbstatin, an inhibitor of EGFR (epidermal growth factor receptor)-associated tyrosine kinase. This erbstatin analog is described to be approximately four times more stable than erbstatin in calf serum. Inhibition of EGFR-associated tyrosine kinase by erbstatin analog in EGFR-overexpressing NIH3T3 cells blocked phenotypic changes in the cells mediated through EGFR activity and delayed EGF-induced DNA synthesis, suggesting use of erbstatin analog as a modifier of EGFR-related malignant phenotypic changes of cells. Erbstatin analog is demonstrated to inhibit autophosphorylation of EGFR and the parent compound is described to inhibit autophosphorylation of the oncogene product p60src in A431 cells. Inhibition of thrombin- and thapsigargin- (sc-24017) induced actin polymerization by erbstatin analog is also described, mediated through inhibition of tyrosine kinases and inhibitory towards store-mediated Ca2+ entry. Erbstatin analog has been further employed as a general inhibitor of tyrosine kinases to identify their activity in various biological processes.
Erbstatin Analog (CAS 63177-57-1) References
- Tyrosine kinases activate store-mediated Ca2+ entry in human platelets through the reorganization of the actin cytoskeleton. | Rosado, JA., et al. 2000. Biochem J. 351 Pt 2: 429-37. PMID: 11023829
- Synthesis and cytotoxicity of some rigid derivatives of methyl 2,5-dihydroxycinnamate. | Nam, NH., et al. 2002. Arch Pharm Res. 25: 590-9. PMID: 12433188
- Inhibition of epidermal growth factor receptor functions by tyrosine kinase inhibitors in NIH3T3 cells. | Umezawa, K., et al. 1992. FEBS Lett. 314: 289-92. PMID: 1468560
- Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors. | Umezawa, K., et al. 1990. FEBS Lett. 260: 198-200. PMID: 2298299
- In situ inhibition of tyrosine protein kinase by erbstatin. | Imoto, M., et al. 1987. Biochem Int. 15: 989-95. PMID: 3501720
- The erbstatin analogue methyl 2,5-dihydroxycinnamate cross-links proteins and is cytotoxic to normal and neoplastic epithelial cells by a mechanism independent of tyrosine kinase inhibition. | Stanwell, C., et al. 1995. Cancer Res. 55: 4950-6. PMID: 7585535
- Alpha 2-adrenoceptor-mediated vasoconstriction requires a tyrosine kinase. | Jinsi, A. and Deth, RC. 1995. Eur J Pharmacol. 277: 29-34. PMID: 7635170
- ADP- and thapsigargin-evoked Ca2+ entry and protein-tyrosine phosphorylation are inhibited by the tyrosine kinase inhibitors genistein and methyl-2,5-dihydroxycinnamate in fura-2-loaded human platelets. | Sargeant, P., et al. 1993. J Biol Chem. 268: 18151-6. PMID: 7688740
- The tyrosine kinase inhibitors, genistein and methyl 2,5-dihydroxycinnamate, inhibit the release of (3H)arachidonate from human platelets stimulated by thrombin or collagen. | Hargreaves, PG., et al. 1994. Thromb Haemost. 72: 634-42. PMID: 7878644
- Inhibition of Abelson oncogene function by erbstatin analogues. | Kawada, M., et al. 1993. Drugs Exp Clin Res. 19: 235-41. PMID: 8013266
- The tyrosine kinase inhibitors methyl 2,5-dihydroxycinnamate and genistein reduce thrombin-evoked tyrosine phosphorylation and Ca2+ entry in human platelets. | Sargeant, P., et al. 1993. FEBS Lett. 315: 242-6. PMID: 8422913
- Inhibition of the G2/M transition of the cell cycle by methyl-2,5-dihydroxycinnamate in human lymphoid cells. | Koch, JA., et al. 1996. Biochem Biophys Res Commun. 225: 531-6. PMID: 8753796
- Inhibition of cytokine-inducible nitric oxide synthase in rat microglia and murine macrophages by methyl-2,5-dihydroxycinnamate. | Zielasek, J., et al. 1996. Neurochem Int. 29: 83-7. PMID: 8808792
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Erbstatin Analog, 5 mg | sc-200511 | 5 mg | $83.00 | |||
Erbstatin Analog, 25 mg | sc-200511A | 25 mg | $305.00 |