PROTAC TRIB2 degrader-1 TFA

PROTAC TRIB2 degrader-1 TFA (5k) (1 nM-3000 nM; 0-24 h) induces potent, dose- and time-dependent degradation of TRIB2 in PC3 prostate cancer cells, with a DC₅₀ of 16.84 nM and a half-maximal degradation time of 5.5 h at a concentration of 500 nM^[1].
PROTAC TRIB2 degrader-1 TFA (1 μM; 0-24 h) induces TRIB2 degradation in H660 and LTL-331R-CL prostate cancer cells^[1].
PROTAC TRIB2 degrader-1 TFA (500 nM; 16 h) induces TRIB2 degradation in PC3 prostate cancer cells via the CRBN-dependent ubiquitin-proteasome pathway, which is evidenced by experimental results that Bortezomib (HY-10227) restores TRIB2 levels while Pomalidomide (HY-10984) inhibits this degradation process^[1].
PROTAC TRIB2 degrader-1 TFA (1 μM; 4 h) is a selective TRIB2 degrader in LTL-331R-CL prostate cancer cells, with extremely weak off-target protein degradation activity^[1].
PROTAC TRIB2 degrader-1 TFA (0-5 days) potently inhibits the proliferation of PC3 and LTL-331R-CL prostate cancer cells, with IC₅₀ values of 30.38 nM and 3.9 nM respectively after 5 days of treatment^[1].

PROTAC TRIB2 degrader-1 TFA (2 μM; 3 h) directly binds to TRIB2 in PC3 prostate cancer cells, which is confirmed by the stability of TRIB2 during heat treatment^[1].
PROTAC TRIB2 degrader-1 TFA (120 min) inhibits the ATP-binding affinity of recombinant human TRIB2 protein in a dose-dependent manner, with an IC₅₀ value of 65.21 nM^[1].

PROTAC TRIB2 degrader-1 TFA (0.5-300 nM; 0-24 h) induces apoptosis in PC3, H660 and LTL-331R-CL prostate cancer cells, which is confirmed by time- and dose-dependent cleavage of PARP^[1].