PP121

PP121 is a potent dual inhibitor of tyrosine and phosphoinositide kinases with IC₅₀ values ranging from 2 to 60 nM for p110α, mTOR, Src, Abl, and VEGFR.¹ It demonstrates >90% inhibition of tyrosine kinases and <50% inhibition of 135 serine/threonine kinases at a concentration of 1 μM in a panel of 200 kinases. PP121 directly inhibits mTOR, PI3K, v-Src, and Bcr-Abl in tumor cells and inhibits proliferation of TT thyroid carcinoma cells (IC₅₀ = 50 nM) in vitro. It blocks VEGF-driven human umbilical vein endothelial cell (HUVEC) tube formation (IC₅₀ = 0.31 nM), an in vitro model of tumor angiogenesis. PP121 also inhibits MEKK2/MAP3K2 (IC₅₀ = 31 nM), a kinase important for tumor growth and metastasis.²

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1. Apsel, B., Blair, J.A., Gonzalez, B., et al. Targeted polypharmacology: Discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat. Chem. Biol. 4(11), 691-699 (2008).

2. Ahmad, S., Johnson, G.L., and Scott, J.E. Identification of ponatinib and other known kinase inhibitors with potent MEKK2 inhibitory activity. Biochem. Biophys. Res. Commun. 463(4), 888-893 (2015).