VRK-IN-1 is a potent and selective inhibitor of vaccinia-related kinases 1 (VRK1), with an IC50 of 150 nM. VRK1 is human Ser/Thr protein kinases associated with increased cell division and neurological disorders[1].
VRK-IN-1 binds to VRK1-FL by enthalpy-driven, with a Kd of 190 nM[1].VRK-IN-1 (0.4-25 μM; 24 h) slightly decreases the viability of human HeLa cells at the concentration of 3.2 μM[1].
[1]. Serafim RAM, et, al. Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2. ACS Med Chem Lett. 2019 Aug 19;10(9):1266-1271.
