An inhibitor of EGF receptor kinase
Tyrphostin 9 is an inhibitor of PDGFR with IC50 value of ~2.5μM [1].
Tyrphostin 9 is generated as specific inhibitor of PDGFR in 1991. It also has inhibitory effect on the proliferation of SMC. Tyrphostin 9 potently inhibits the PDGF-dependent SMC proliferation with IC50 value of 40nM and inhibits the PDGF-dependent autophosphorylation of PDGFR with IC50 value of ~2.5μM. Besides that, Tyrphostin 9 also affects the phosphorylation of PLCγ (IC50 value of about 2.5μM) and the PDGF-dependent c-fos expression. Moreover, Tyrphostin 9 is found to be an inhibitor of EGFR with IC50 value of 460μM [1, 2].
In the rat carotid artery injury model, treatment of Tyrphostin 9 significantly reduces neointimal hyperplasia through inhibiting the tyrosine phosphorylation in injured arteries [1].
参考文献:
[1] Levitzki A. PDGF receptor kinase inhibitors for the treatment of restenosis. Cardiovascular research, 2005, 65(3): 581-586.
[2] Levitzki A. Tyrphostins—potential antiproliferative agents and novel molecular tools. Biochemical pharmacology, 1990, 40(5): 913-918.
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