PIN1 degrader-2

PIN1 degrader-2 (164A10) (pre-incubated for 6 hours; followed by an additional 2-hour incubation) potently binds to purified human Pin1 in the DELFIA assay, with an IC₅₀ value of 4.1 nM^[1].
PIN1 degrader-2 (40 μM; PIN1 20 μM; 10 min; 10 °C) induces a decrease in the thermal stability of PIN1, with a ΔT_m of -8.95 °C^[1].
PIN1 degrader-2 (5 or 15 μM; 24 h) significantly reduces PIN1 protein levels in BxPC3 cells, with normalized PIN1/actin ratios of approximately 11% and 2%, respectively^[2].
PIN1 degrader-2 (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; the normalized PIN1/actin ratios are approximately 8%, 9%, 5%, 15%, 22% and 24% at 15 μM^[1].
PIN1 degrader-2 (5 μM; 24 h) induces PIN1 degradation in BxPC3 cells; the proteasome inhibitors BTZ (50 nM) and CFZ (1 μM) significantly rescue this degradation, whereas the autophagy inhibitors Baf A1 (100 nM) and HCQ (25 μM) exert no such effective rescuing effect^[1].
The crystal structure of PIN1 degrader-2 in complex with PIN1 R14A reveals continuous electron density between 164A10 and PIN1 Cys113, confirming the covalent modification of Cys113 by PIN1 degrader-2 (PDB ID: 8VJG)^[1].
PIN1 degrader-2 (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 16.6, 7.4, 5.8, 23.0, 22.2, approximately 30 and >20 μM^[1], respectively.

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