STK16-IN-1

Description: STK16-IN-1 is a novel and highly selective ATP competitive inhibitor of STK16 kinase with an IC50 of 295 nM. STK16 is a serine/threonine protein kinase that is ubiquitously expressed and is conserved among all eukaryotes. STK16 has been implicated to function in a variety of cellular processes such as VEGF and cargo secretion, but the pathways through which these effects are mediated remain to be elucidated. STK16-IN-1 exhibits potent inhibitory activity against STK16 kinase (IC50: 0.295 uM) with excellent selectivity across the kinome as assessed using the KinomeScan profiling assay (S score (1) = 0.0). In MCF-7 cells, treatment with STK16-IN-1 results in a reduction in cell number and accumulation of binucleated cells, which can be recapitulated by RNAi knockdown of STK16. Co-treatment of STK16-IN-1 with chemotherapeutics such as cisplatin, doxorubicin, colchicine, and paclitaxel results in a slight potentiation of the antiproliferative effects of the chemotherapeutics. STK16-IN-1 provides a useful tool compound for further elucidating the biological functions of STK16.

References: ACS Chem Biol. 2016 Jun 17; 11(6):1537-43.