1223001-53-3

STK16-IN-1 is a highly selective STK16 kinase inhibitor.

STK16-IN-1 is a cell-permeable pyrrolonaphthyridinone compound th at acts as an ATP-competitive inhibitor against NAK (Numb Associated Kinase) family serine/threonine kinase STK16 (IC50/substrate = 0.91 μM/4EBP1 and 1.2 μM/DRG1[ATP] = 20 μM) with excellent selectivity over a panel of 378 kinases. Despite its inhibitory potency against PI 3-Ks (IC50 = 1.070.8560.867 μM against p110α/p85αp110δ/p85αp110γ respectively) in cell-free assaysSTK16-IN-1 is ineffective against their cellular activity up to 10 μM concentration. STK16-IN-1 treatment (10 μM for 72 hrs) is shown to cause cell number reduction (~50% in HCT-116 and MCF-7 cultures)as well as increased populations of binucleated cells (~5-fold in MCF-7 culture) and G2/M cells (~7 and 3-fold in HCT-116 and MCF-7 culturesrespectively) in an STK16-dependent manner. A useful tool for elucidating STK16 biological functions.