GK241 is a secretory phospholipase A2 (sPLA2) (Type IIA) inhibitor (IC50s = 0.143 and 0.068 µM for the human and mouse enzymes, respectively).1,2 It inhibits IL-1β-induced production of prostaglandin E2 in isolated rat renal mesangial cells when used at concentrations of 3 and 10 µM.3 GK241 also inhibits the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), also known as 3C-like protease (3CLpro; IC50 = 24 µM).1
1.Theodoropoulou, M.A., Koutoulogenis, G.S., Zhang, L., et al.Identification of a dual inhibitor of secreted phospholipase A2 (GIIA sPLA2) and SARS-CoV-2 main proteasePharmaceuticals (Basel)15(8)961(2021) 2.Vasilakaki, S., Barbayianni, E., Leonis, G., et al.Development of a potent 2-oxoamide inhibitor of secreted phospholipase A2 guided by molecular docking calculations and molecular dynamics simulationsBioorg. Med. Chem.24(8)1683-1695(2016) 3.Vasilakaki, S., Barbayianni, E., Magrioti, V., et al.Inhibitors of secreted phospholipase A2 suppress the release of PGE2 in renal mesangial cellsBioorg. Med. Chem.24(13)3029-3034(2016)