PIN1 degrader-1

PIN1 degrader-1 (compound 158H9) (pre-incubated for 6 h followed by a 2 h incubation) inhibits the binding of PIN1 to biotinylated D-peptide in the DELFIA displacement assay, with an IC₅₀ of 21.5 nM^[1].

PIN1 degrader-1 (40 μM; PIN1 20 μM; 10 min; 10 °C) induces a decrease in the thermal stability of PIN1, with a ΔT_m of -8.41 °C^[1].

PIN1 degrader-1 (5 or 15 μM; 24 h) significantly reduces PIN1 protein levels in BxPC3 cells, with normalized PIN1/actin ratios of approximately 6% and 3%, respectively^[2].
PIN1 degrader-1 (0.5-15 μM; 24 h) reduces PIN1 protein levels in a concentration-dependent manner in BxPC3, MIA PaCa-2, PANC-1, MDA-MB-231, PC3 and A549 NucLight Red cells; at 15 μM, the normalized PIN1/actin ratios are approximately 2%, 3%, 1%, 7%, 12% and 4%, respectively^[1].
PIN1 degrader-1 (5 μM; 24 h) induces PIN1 degradation in BxPC3 cells; the proteasome inhibitors BTZ (50 nM) and CFZ (1 μM) can rescue this degradation, whereas the autophagy inhibitors Baf A1 (100 nM) and HCQ (25 μM) exert no effective rescue effect^[1].
PIN1 degrader-1 reduces PIN1 protein levels in a time-dependent manner in BxPC3 cells; BTZ can essentially rescue PIN1 degradation within approximately 14 h, after which its rescue effect gradually weakens^[1].
PIN1 degrader-1 (72 h) reduces the cell viability of BxPC3, MIA PaCa-2, PANC-1, MDA-MB-231, PC3, A549 and KPC cells, with EC₅₀ values of 7.5, 13.6, 15.8, 15.1, 15.6, approximately 26 and >35 μM^[1], respectively.