Bioactivity | 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]. | ||||||||||||
Target | IC50: 150 nM (VRK1) | ||||||||||||
Invitro | 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]. | ||||||||||||
Name | VRK-IN-1 | ||||||||||||
CAS | 2378855-09-3 | ||||||||||||
Formula | C18H11F4NO2 | ||||||||||||
Molar Mass | 349.28 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |