In vitro
CYC116, the most aurora-selective aurora kinase inhibitors, can inhibit aurora A and B kinases about 50-fold more potently than any of the CDKs assayed. CYC116 inhibits two tyrosine kinases, FMS-like tyrosine kinase 3 (FLT3) and vascular endothelial growth factor receptor 2 kinase (VEGFR2), with a Ki value of 44 nM. CYC116 shows no inhibition to PKA, Akt/PKB, PKC, GSK-3alpha, GSK-3beta, ERK2, CaMKII, CK2, Plk1 and SAPK2A. CYC116 shows low micromolar activity against 70 kDa ribosomal protein S6 kinase (p70S6K), Src, and lymphocyte-specific protein tyrosine kinase (Lck). CYC116 is particularly cytotoxic against the acute myelogenous leukemia cell line MV4-11. Treatment with 1.25 uM CYC116 for 7 h results in complete inhibition of histone H3 phosphorylation. CYC116 inhibits autophosphorylation of both aurora A and B(66) at antiproliferative concentrations in cells.
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