BQZ-485

BQZ-485 (compound 1) (0.1-10 μM; 48 h) potently inhibits the proliferation of human prostate cancer cell line PC-3, with an IC₅₀ value of 0.57 μM^[1].
BQZ-485 stabilizes the bindable and purified wild-type GDI2 protein; it directly binds to the purified GDI2 protein with a K_D value of 46 μM^[1].
BQZ-485 binds to domain I within the Rab-binding platform of GDI2, with a key interaction occurring with the Tyr245 residue; it inhibits the GDI2-Rab1A interaction in a NanoLuc-based cell-free assay, with an IC₅₀ of 6.85 μM; it can inhibit GDI2^WT-mediated retrieval of Rab1A from membranes, with an EC₅₀ of 4.96 μM^[1].
BQZ-485 (2 μM; 24 h) disrupts the subcellular distribution of Rab1A in human prostate cancer cell line PC-3, reducing cytoplasmic Rab1A while increasing membrane-bound Rab1A; it can disrupt the interaction between endogenous GDI2 and Rab1A in human prostate cancer cell line PC-3 expressing wild-type GDI2^[1].
BQZ-485 (1 μM; 8 h, 0-720 min) induces endoplasmic reticulum-derived cytoplasmic vacuolization and paraptotic cell death in human prostate cancer cells PC-3^[1].
BQZ-485 (1 μM; 24 h) induces endoplasmic reticulum stress and activates the unfolded protein response in human prostate cancer PC-3 cells, which is characterized by increased expression levels of GRP78, CHOP and p-eIF2α^[1].

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