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Tyrphostin A25 (CAS 118409-58-8)

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Alternate Names:
Tyrphostin 25; RG-50875; NSC 676484; Tyrphostin AG-82
Application:
Tyrphostin A25 is a cell-permeable, reversible, and competitive protein tyrosine kinase (PTK) substrate inhibitor
CAS Number:
118409-58-8
Purity:
≥95%
Molecular Weight:
202.16
Molecular Formula:
C10H6N2O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Tyrphostin A25 is a cell-permeable, competitive and reversible inhibitor of substrate binding on protein tyrosine kinases. In cultured rat hepatocytes, Tyrphostin A25 may act to inhibit endocytosis of tyramine-cellobiose-asialoorosomucoid (TC-AOM). It has also shown to inhibit neuromedin B-induced phosphorylation of focal adhesion kinase (p125FAK). Furthermore, it inhibits EGFR (epidermal growth factor receptor) tyrosine kinase (IC50=3 µM) and the GTPase activity of transducin. In small cell lung cancer cells, Tyrphostin A25 has been observed to obstruct neuropeptide and basal stimulated growth. In addition, it has blocked the induction of inducible NO synthase in glial cells and induced apoptosis in human leukemic cell lines.


Tyrphostin A25 (CAS 118409-58-8) References

  1. Inhibition of ovulation by tyrosine kinase inhibitors in the in vitro perfused rat ovary.  |  Matousek, M., et al. 1999. J Reprod Fertil. 117: 379-85. PMID: 10690206
  2. Genistein, a soybean isoflavone, inhibits inward rectifier K(+) channels in rat osteoclasts.  |  Okamoto, F., et al. 2001. Jpn J Physiol. 51: 501-9. PMID: 11564287
  3. Tyrphostins are inhibitors of guanylyl and adenylyl cyclases.  |  Jaleel, M., et al. 2004. Biochemistry. 43: 8247-55. PMID: 15209521
  4. A new type of protein methylation activated by tyrphostin A25 and vanadate.  |  Miranda, TB., et al. 2004. FEBS Lett. 577: 181-6. PMID: 15527782
  5. S-adenosylmethionine-dependent protein methylation in mammalian cytosol via tyrphostin modification by catechol-O-methyltransferase.  |  Lipson, RS. and Clarke, SG. 2007. J Biol Chem. 282: 31094-102. PMID: 17724020
  6. Tyrphostins inhibit PDGF-induced DNA synthesis and associated early events in smooth muscle cells.  |  Bilder, GE., et al. 1991. Am J Physiol. 260: C721-30. PMID: 1850195
  7. Regulation of wild-type and mutant KCNQ1/KCNE1 channels by tyrosine kinase.  |  Missan, S., et al. 2009. Pflugers Arch. 458: 471-80. PMID: 19139916
  8. Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.  |  Gazit, A., et al. 1989. J Med Chem. 32: 2344-52. PMID: 2552117
  9. Blocking of EGF-dependent cell proliferation by EGF receptor kinase inhibitors.  |  Yaish, P., et al. 1988. Science. 242: 933-5. PMID: 3263702
  10. Inhibition of autophagy and multiple steps in asialoglycoprotein endocytosis by inhibitors of tyrosine protein kinases (tyrphostins).  |  Holen, I., et al. 1995. J Biol Chem. 270: 12823-31. PMID: 7759538
  11. Inhibition of GTP-utilizing enzymes by tyrphostins.  |  Wolbring, G., et al. 1994. J Biol Chem. 269: 22470-2. PMID: 7915715
  12. Inhibitors of tyrosine phosphorylation induce apoptosis in human leukemic cell lines.  |  Bergamaschi, G., et al. 1993. Leukemia. 7: 2012-8. PMID: 8255101
  13. Antiproliferative effect of tyrosine kinase inhibitors in epidermal growth factor-stimulated growth of human gastric cancer cells.  |  Piontek, M., et al. 1993. Anticancer Res. 13: 2119-23. PMID: 8297123
  14. Neuropeptides stimulate tyrosine phosphorylation and tyrosine kinase activity in small cell lung cancer cell lines.  |  Tallett, A., et al. 1996. Peptides. 17: 665-73. PMID: 8804078
  15. Neuromedin B receptor activation causes tyrosine phosphorylation of p125FAK by a phospholipase C independent mechanism which requires p21rho and integrity of the actin cytoskeleton.  |  Tsuda, T., et al. 1997. Biochemistry. 36: 16328-37. PMID: 9405068

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Tyrphostin A25, 5 mg

sc-3555A
5 mg
$68.00

Tyrphostin A25, 25 mg

sc-3555
25 mg
$282.00