Date published: 2025-12-1

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Tyrphostin 51 (CAS 122520-90-5)

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Alternate Names:
Tyrphostin A51; 2-amino-4-(3,4,5-trihydroxyphenyl)-1,3-butadiene-1,1,3-tricarbonitrile; AG-183
Application:
Tyrphostin 51 is a potent inhibitor of EGFRK activity showing mixed competitive inhibition with ATP and substrate1-3.
CAS Number:
122520-90-5
Purity:
≥98%
Molecular Weight:
268.23
Molecular Formula:
C13H8N4O3
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 51 is a potent inhibitor of EGFR (EGF receptor) kinase activity (IC50=0.8 μM). Inhibition is mixed competitive with ATP and substrate.


Tyrphostin 51 (CAS 122520-90-5) References

  1. Mechanism of ATP-induced [Ca(2+)](i) mobilization in rat basilar smooth muscle cells.  |  Aoki, K., et al. 2000. Stroke. 31: 1377-84; discussion 1384-5. PMID: 10835460
  2. H(2)O(2)-induced egr-1, fra-1, and c-jun gene expression is mediated by tyrosine kinase in aortic smooth muscle cells.  |  Jin, N., et al. 2000. Free Radic Biol Med. 29: 736-46. PMID: 11053775
  3. [Protein tyrosine kinase activation in the repair of rat gastric mucosa after damage].  |  Zeng, J., et al. 1999. Zhonghua Yi Xue Za Zhi. 79: 934-7. PMID: 11715511
  4. Stimulation of L-type Ca(2+) channels by increase of intracellular InsP3 in rat retinal pigment epithelial cells.  |  Mergler, S. and Strauss, O. 2002. Exp Eye Res. 74: 29-40. PMID: 11878816
  5. Calcium influx induced by activation of receptor tyrosine kinases in SV40-transfected human corneal endothelial cells.  |  Mergler, S., et al. 2003. Exp Eye Res. 77: 485-95. PMID: 12957147
  6. Hydrogen peroxide-induced extracellular signal-regulated kinase activation in cultured feline ileal smooth muscle cells.  |  Song, HJ., et al. 2005. J Pharmacol Exp Ther. 312: 391-8. PMID: 15328380
  7. Epidermal growth factor receptor inhibition by tyrphostin 51 induces apoptosis in luteinized granulosa cells.  |  Khan, SM., et al. 2005. J Clin Endocrinol Metab. 90: 469-73. PMID: 15494464
  8. IL-1beta activates p44/42 and p38 mitogen-activated protein kinases via different pathways in cat esophageal smooth muscle cells.  |  Lee, TS., et al. 2006. World J Gastroenterol. 12: 716-22. PMID: 16521184
  9. Signaling mechanisms of sphingosine 1-phosphate-induced ERK1/2 activation in cultured feline esophageal smooth muscle cells.  |  Chung, FY., et al. 2008. Arch Pharm Res. 31: 1437-45. PMID: 19023540
  10. Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.  |  Gazit, A., et al. 1989. J Med Chem. 32: 2344-52. PMID: 2552117
  11. Blocking of EGF-dependent cell proliferation by EGF receptor kinase inhibitors.  |  Yaish, P., et al. 1988. Science. 242: 933-5. PMID: 3263702
  12. Bicyclic compounds as ring-constrained inhibitors of protein-tyrosine kinase p56lck.  |  Burke, TR., et al. 1993. J Med Chem. 36: 425-32. PMID: 8474097

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Tyrphostin 51, 5 mg

sc-200545
5 mg
$59.00

Tyrphostin 51, 25 mg

sc-200545A
25 mg
$305.00