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Chemical Compound Review

Tyrphostin 47     (E)-3-amino-2-[(Z)-(3- hydroxy-4-oxo-1...

Synonyms: Tyrphostin A47, Lopac-T-7540, Tocris-0503, AC1NUNYH, AG213, ...
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Disease relevance of AG 213


High impact information on AG 213

  • The protein tyrosine kinase inhibitor tyrphostin RG50864, which blocks EGF-dependent cell proliferation, blocked EGF-induced tyrosine phosphorylation of PLC-II, its association with EGF receptor, and EGF-induced Ca2+ release [3].
  • Induction of mitogenesis was not the major contribution of bFGF and VEGF165 because the cell number did not change significantly in the presence of TNFalpha, and tyrphostin A47, which inhibited mitosis completely, reduced the formation of tubular structures only by 28-36% [4].
  • When cultures were subjected to E fields in the presence of a tyrosine kinase inhibitor, tyrphostin RG-50864, cathodal AChR clustering was abolished with a half maximal inhibitory dosage of 50 microM [5].
  • Continuous infusion of RG-50864, an inhibitor of EGF receptor kinase activity, at the site of injury prevented the advancement of puberty induced by the lesion [6].
  • Herbimycin A also reduced PAI-1 synthesis, but several other tyrosine protein kinase inhibitors, namely tyrphostin A47, methyl-2,5-dihydroxy-cinnamate, and compound 5, were unable to do so [7].

Biological context of AG 213


Anatomical context of AG 213


Associations of AG 213 with other chemical compounds


Gene context of AG 213


  1. Activation of complement receptor 3 on human monocytes by cross-linking of very-late antigen-5 is mediated via protein tyrosine kinases. van den Berg, B.M., van Furth, R., Hazenbos, W.L. Immunology (1999) [Pubmed]
  2. Effects of receptor tyrosine kinase inhibitor A47 on estrogen and growth factor-dependent breast cancer cell proliferation and apoptosis in vitro. Turbov, J.M., Twaddle, G.M., Yang, X., Liu, N.M., Murthy, S. Journal of surgical oncology. (2002) [Pubmed]
  3. EGF induces tyrosine phosphorylation of phospholipase C-II: a potential mechanism for EGF receptor signaling. Margolis, B., Rhee, S.G., Felder, S., Mervic, M., Lyall, R., Levitzki, A., Ullrich, A., Zilberstein, A., Schlessinger, J. Cell (1989) [Pubmed]
  4. Cooperative effect of TNFalpha, bFGF, and VEGF on the formation of tubular structures of human microvascular endothelial cells in a fibrin matrix. Role of urokinase activity. Koolwijk, P., van Erck, M.G., de Vree, W.J., Vermeer, M.A., Weich, H.A., Hanemaaijer, R., van Hinsbergh, V.W. J. Cell Biol. (1996) [Pubmed]
  5. A role of tyrosine phosphorylation in the formation of acetylcholine receptor clusters induced by electric fields in cultured Xenopus muscle cells. Peng, H.B., Baker, L.P., Dai, Z. J. Cell Biol. (1993) [Pubmed]
  6. Transforming growth factor alpha contributes to the mechanism by which hypothalamic injury induces precocious puberty. Junier, M.P., Ma, Y.J., Costa, M.E., Hoffman, G., Hill, D.F., Ojeda, S.R. Proc. Natl. Acad. Sci. U.S.A. (1991) [Pubmed]
  7. Genistein reduces tumor necrosis factor alpha-induced plasminogen activator inhibitor-1 transcription but not urokinase expression in human endothelial cells. van Hinsbergh, V.W., Vermeer, M., Koolwijk, P., Grimbergen, J., Kooistra, T. Blood (1994) [Pubmed]
  8. Quantitative dissociation between EGF effects on c-myc and c-fos gene expression, DNA synthesis, and epidermal growth factor receptor tyrosine kinase activity. Hauguel-DeMouzon, S., Csermely, P., Zoppini, G., Kahn, C.R. J. Cell. Physiol. (1992) [Pubmed]
  9. Inhibition of human neutrophil responses by alpha-cyano-3,4-dihydroxythiocinnamamide; a protein-tyrosine kinase inhibitor. Dryden, P., Duronio, V., Martin, L., Hudson, A.T., Salari, H. Br. J. Pharmacol. (1992) [Pubmed]
  10. Tyrosine kinases are required for IFN-gamma-induced growth of human embryonic forebrain astrocytes. Mousa, A., Seiger, A., Bakhiet, M. Neuroreport (1998) [Pubmed]
  11. Tyrosine kinase inhibitors as antiproliferative agents against an estrogen-dependent breast cancer cell line in vitro. Twaddle, G.M., Turbov, J., Liu, N., Murthy, S. Journal of surgical oncology. (1999) [Pubmed]
  12. Endogenous epidermal growth factor regulates limb development. Canoun, C., Ma, C., Halpern, D., Shum, L., Bringas, P., Sank, A., Slavkin, H.C. J. Surg. Res. (1993) [Pubmed]
  13. Tyrosine kinase activity, cytoskeletal organization, and motility in human vascular endothelial cells. Romer, L.H., McLean, N., Turner, C.E., Burridge, K. Mol. Biol. Cell (1994) [Pubmed]
  14. Epidermal growth factor receptor signaling cascade as target for tyrphostin (RG 50864) in epithelial cells. Paradoxical effects on mitogen-activated protein kinase kinase and mitogen-activated protein kinase activities. Nowak, F., Jacquemin-Sablon, A., Pierre, J. Biochem. Pharmacol. (1997) [Pubmed]
  15. Epidermal growth factor-specific protein tyrosine phosphorylation in preimplantation embryo development. Paria, B.C., Tsukamura, H., Dey, S.K. Biol. Reprod. (1991) [Pubmed]
  16. Tyrphostin-A47 inhibitable tyrosine phosphorylation of flagellar proteins is associated with distinct alteration of motility pattern in hamster spermatozoa. Mariappa, D., Siva, A.B., Shivaji, S., Seshagiri, P.B. Mol. Reprod. Dev. (2006) [Pubmed]
  17. Antigen- and ionophore-induced signal transduction in rat basophilic leukemia cells involves protein tyrosine phosphorylation. Yu, K.T., Lyall, R., Jariwala, N., Zilberstein, A., Haimovich, J. J. Biol. Chem. (1991) [Pubmed]
  18. Effects of calcium, calmodulin, protein kinase C and protein tyrosine kinases on volume-activated taurine efflux in human erythroleukemia cells. Huang, C.C., Chang, C.B., Liu, J.Y., Basavappa, S., Lim, P.H. J. Cell. Physiol. (2001) [Pubmed]
  19. Signal transduction for interleukin-3-dependent leukotriene synthesis in normal human basophils: opposing role of tyrosine kinase and protein kinase. Krieger, M., von Tscharner, V., Dahinden, C.A. Eur. J. Immunol. (1992) [Pubmed]
  20. Activation of the mitogen-activated protein kinase cascade by tyrphostin (RG 50864). Agbotounou, W.K., Mousset, S., Piperno, S., Pierre, M., Jacquemin-Sablon, A., Pierre, J. Biochem. Pharmacol. (1994) [Pubmed]
  21. Protein binding modulates inhibition of the epidermal growth factor receptor kinase and DNA synthesis by tyrphostins. Hoffman, R., Dennis, I.F., Donaldson, J. Cancer Chemother. Pharmacol. (1995) [Pubmed]
  22. Presynaptic differentiation induced in cultured neurons by local application of basic fibroblast growth factor. Dai, Z., Peng, H.B. J. Neurosci. (1995) [Pubmed]
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