JLJ648 is a Gag-Pol dimerizer with antiviral activity. JLJ648 can inhibit HIV replication and induce infected cell pyroptosis. JLJ648 can be used for the research of infection, such as HIV (human immunodeficiency virus) [1].
In Vitro, JLJ648 (3 days) inhibits HIV-1 replication in MT-2 cells with an EC50 of 1.6 nM[1]. JLJ648 shows low cytotoxicity in MT-2 and THP-1 cells (CC50>100 μM) and a CC50 of 22.9 μM in primary CD4+ T cells[1]. JLJ648 (17 h) promotes the homodimerization of recombinant HIV-1 RT p66 subunit with an EC50 of 95 nM[1]. JLJ648 (3-4 h) induces HIV protease-dependent pyroptosis in THP-1 clone14 cells and HIV-infected primary CD4+ T cells, with an EC50 of 86 nM[1]. JLJ648 (50 μM, 12 h) binds to HIV-1 RT p66 to form two oligomeric structures, subunits in catalytic/structural conformations and "infinity knot"-shaped homotetramer[1].
References:
[1]. Hollander K, et al. Mechanistic basis for a novel dual-function Gag-Pol dimerizer potentiating CARD8 inflammasome activation and clearance of HIV-infected cells. NPJ Drug Discov. 2025;2(1):22.
In Vitro, JLJ648 (3 days) inhibits HIV-1 replication in MT-2 cells with an EC50 of 1.6 nM[1]. JLJ648 shows low cytotoxicity in MT-2 and THP-1 cells (CC50>100 μM) and a CC50 of 22.9 μM in primary CD4+ T cells[1]. JLJ648 (17 h) promotes the homodimerization of recombinant HIV-1 RT p66 subunit with an EC50 of 95 nM[1]. JLJ648 (3-4 h) induces HIV protease-dependent pyroptosis in THP-1 clone14 cells and HIV-infected primary CD4+ T cells, with an EC50 of 86 nM[1]. JLJ648 (50 μM, 12 h) binds to HIV-1 RT p66 to form two oligomeric structures, subunits in catalytic/structural conformations and "infinity knot"-shaped homotetramer[1].
References:
[1]. Hollander K, et al. Mechanistic basis for a novel dual-function Gag-Pol dimerizer potentiating CARD8 inflammasome activation and clearance of HIV-infected cells. NPJ Drug Discov. 2025;2(1):22.