Bioactivity | STK16-IN-1 is a STK16 kinase inhibitor with an IC50 of 295 nM. | ||||||||||||
Target | IC50: 295 nM (STK16) | ||||||||||||
Invitro | 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]. | ||||||||||||
Name | STK16-IN-1 | ||||||||||||
CAS | 1223001-53-3 | ||||||||||||
Formula | C17H12FN3O | ||||||||||||
Molar Mass | 293.30 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Liu F, et al. Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem Biol. 2016 Jun 17;11(6):1537-43. |