KP372-1 directly inhibits the kinase activities of Akt, PDK1 and Flt3 (Fms-like tyrosine kinase 3), which are aberrantly activated in acute myelogenous leukemia (AML). It is a cell permeant inhibitor that decreases the colony-forming ability of AML cells (IC50 < 200 nM) with minimal cytoxic effects on normal hematopoietic progenitor cells. KP372-1 has also been shown to suppress cell proliferation and induce apoptosis in thyroid cancer cells and gliobastoma. Provided as a 1:1 mixture of regioisomers.
1) M. Mandal et al. “The Akt Inhibitor KP372-1 Suppresses Akt Activity and Cell Proliferation and Induces Apoptosis in Thyroid Cancer Cells” Br. J. Cancer, 2005, 92, 1899-1905.
2) Z. Zeng et al “Simultaneous Inhibition of PDK1/AKT and Fms-Like Tyrosine Kinase 3 Signaling by a Small-Molecule KP372-1 Induces Mitochondrial Dysfunction and Apoptosis in Acute Myelogenous Leukemia.” Cancer Res., 2006, 66, 3737-3746.