Oxindole I is a potent and selective inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinase Flk-1 (fetal liver kinase-1; IC50 = 390 nM). Also, to a lesser extent, it inhibits PDGFR (platelet derived growth factor receptor) kinase (IC50 = 12 μM). However, Oxindole I does not affect EGFR, HER2, and IGF-1R even at high concentrations (>100 μM). Oxindole I also inhibits cyclin D1/Cdk4 enzyme (IC50 = 4.9 μM) preferentially over cyclin E/Cdk2 (IC50 = 10 μM) and cyclin B/Cdk1 (IC50 = 10.2 μM).
1. Kent, L L., et al., 1999. Characterization of novel inhibitors of cyclin-dependent kinases. Biochemical and biophysical research communications. 260(3): 768-74. PMID: 10403840
2. Vieth, M., et al., 2000. DoMCoSAR: a novel approach for establishing the docking mode that is consistent with the structure-activity relationship. Application to HIV-1 protease inhibitors and VEGF receptor tyrosine kinase inhibitors. Journal of medicinal chemistry. 43(16): 3020-32. PMID: 10956210