PROTAC CG167

PROTAC CG167 binds to purified full-length human CypA with a K_D of 64 nM, and to N-terminally truncated human CypB with a K_D of 71 nM^[1].
PROTAC CG167 (0.01-10 μM; 1 h-6 days) degrades CypA in Jurkat human T cells in a time- and dose-dependent manner via a VHL-dependent, neddylation-dependent PROTAC mechanism, with a DC₅₀ of 123 nM and a D_max of 76% at 48 h^[1].
PROTAC CG167 (5 μM; 72 h) selectively degrades CypA in the human monocytic cell line THP-1, causing only slight reductions in CypH and CypE levels, with no significant effects on other members of the cyclophilin family^[1].
PROTAC CG167 (5 μM; 48 h) degrades CypA in various human cell lines and primary cells, with differences in degradation efficiency observed across different cell types, and exhibits higher selectivity for CypA over CypB^[1].
PROTAC CG167 (1-5 μM; 48 h) exhibits better anti-HIV-1 and anti-HCV activity than its parent inhibitor TWH106 at a low concentration (1 μM) in primary activated human CD4⁺ T cells and Huh7 human hepatocellular carcinoma cells, and this activity depends on VHL-mediated CypA degradation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.