GSK3326595

GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma^{[1][2][3][4][5]}. IC50 & Target:IC50: 6.2 nM (PRMT5)^[1] In Vitro:GSK3326595 (10-100 nM, 24-72 h) inhibits SARS-CoV-2spike pseudovirus infection HEK-293 cells and A549 cells by attenuating ACE2-RBD interaction^[1].
GSK3326595 (100 nM, 12 h) primes peritoneal macrophages to IFN-gamma-induced M1 polarization^[3].
GSK3326595 (0.15-10 μM, 72 h) induces cell death in MCL cell^[4]. In Vivo:GSK3326595 (5 mg/kg, Intraperitoneal injection, three times a week for 9 weeks) increased hepatic triglyceride levels without affecting atherosclerosis in LDL receptor knockout mice^[3]. GSK3326595 (25-50 mg/kg, Oral, once a day for 2 weeks) enhances the efficacy of anti-programed cell death protein 1 (PD-1) immune checkpoint therapy (ICT) in hepatocellular carcinoma (HCC) in myelocytomatosis transgene turned on (MYC-ON) mice^[5].