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).
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PMID: # 26188358 Zhou, W. et al. 2015. Oncotarget. 6: 21557-71.
PMID: # 25186293 Soggia, A. et al. 2014. Diabetologia. 57: 2348-56.