a-Cyano-(3,4-dihydroxy)cinnamoyl-(3′,4′-dihydroxyphenyl)ketone Tyrphostin AG 538 Dark yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A potent, competitive inhibitor of IGF-1 receptor kinase (IC50 = 400 nM). Reaction is competitive with respect to IGF-1R substrate. Also inhibits the phosphorylation of PTK substrate poly(Glu,Tyr) by IGF-1R, IR, EGF-R, and Src (IC50 = 60 nM, 113 nM, 370 nM, and 2.4 µM, respectively). Inhibits the phosphorylation of PKB at a much higher concentration (IC50 = 76 µM). Purity: ≥95% by HPLC. CAS 133550-18-2. Ref.: Blum, G., et al. 2000. Biochemistry 39, 15705. |