PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. It exhibits anti-proliferative effects, induces apoptosis, inhibits NF-κB activity, and causes cell cycle arrest at the G1 phase. PROTAC XPO1 degrader-1 is applicable to research on hematological malignancies.

PROTAC XPO1 degrader-1 (Compound 2c) effectively degrades XPO1 protein in MV4-11 acute myeloid leukemia (AML) cells with a DC50 of 23.67 nM [1]. It exhibits significant anti-proliferative effects, showing IC50 values of 0.142 μM for MV4-11 cells and 0.186 μM for MOLM-13 cells [1]. At concentrations of 100-500 nM over 24 hours, it induces apoptosis in MV4-11 cells via the caspase pathway [1]. When applied at 100-200 nM for 24 hours, it arrests the cell cycle at the G1 phase in MV4-11 cells [1]. Additionally, 50 nM of PROTAC XPO1 degrader-1 for 24 hours reduces cell migration in MV4-11 cells [1].