STK16-IN-1

• CAT Number: I011364
• CAS Number: 1223001-53-3
• Molecular Formula: C17H12FN3O
• Molecular Weight: 293.30
• Purity: ≥95%
• Synonyms: 1-(4-fluoro-3-methylphenyl)-7H-pyrrolo[2,3-h][1,6]naphthyridin-2-one
• InChI: InChI=1S/C17H12FN3O/c1-10-8-12(3-4-14(10)18)21-15(22)5-2-11-9-20-17-13(16(11)21)6-7-19-17/h2-9H,1H3,(H,19,20)
• InChIKey: WQNRDXHKVSKUPI-UHFFFAOYSA-N
• SMILES: CC1=C(C=CC(=C1)N2C(=O)C=CC3=CN=C4C(=C32)C=CN4)F

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].

Reference

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