Background:

STK16-IN-1 is a STK16 kinase inhibitor with an IC50 of 295 nM.

STK16-IN-1, which exhibits potent inhibitory activity against STK16 kinase (IC50=0.295 μM) with excellent selective across the kinome as assessed using the KinomeScanTM profiling assay. STK16-IN-1 inhibits mTOR kinase with an IC50 of 5.56 μM. 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 anti-proliferative effects of the chemotherapeutics. STK16-IN-1 provides a useful tool compound for further elucidating the biological functions of STK16)[1].

[1]. Liu F, et al. Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem Biol. 2016 Jun 17;11(6):1537-43.