PROTAC HIV-1 degrader-1

PROTAC HIV-1 degrader-1 (VHL-3) potently inhibits the replication of HIV-1_IIIB in MT-4 cells, with an EC₅₀ value of 3.0 nM^[1].
PROTAC HIV-1 degrader-1 potently inhibits the replication of HIV-1NL4-3 in MT-4 cells, with a full-cycle EC₅₀ of 1.17 nM, and its activity in the early stage (EC₅₀ = 0.91 nM) is stronger than that in the late stage (EC₅₀ = 3.68 nM)^[1].
PROTAC HIV-1 degrader-1 potently inhibits the replication of LEN (HY-111964)-resistant HIV-1 mutants in MT-4 cells, with an EC₅₀ value of 21 nM against N74D, 2.1 nM against K70R, and 19 nM against A105T^[1].
PROTAC HIV-1 degrader-1 (0-2 μM; 2-24 h) degrades early and late stage HIV-1 CA in HEK293T cells in a dose- and time-dependent manner, with DC₅₀ values of 812 nM and 252 nM, respectively^[1].
PROTAC HIV-1 degrader-1 (1-5 μM) degrades HIV-1 CA in HEK293T cells via the ubiquitin-proteasome pathway dependent on VHL E3 ligase recruitment^[1].
PROTAC HIV-1 degrader-1 degrades LEN-resistant HIV-1 CA mutants N74D and K70R in HEK293T cells, but fails to degrade A105T^[1].
PROTAC HIV-1 degrader-1 (10 μM) competes with host factors CPSF6 and Sec24C for binding to HIV-1 CA, and prevents their association with assembled CA structures^[1].

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