fkbp52

ILS-920 is a Rapamycin analog characterized by diminished immunosuppressive effects but remarkable neuroprotective properties. It exhibits selective binding affinity towards the immunophilin FKBP52 as well as the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 displays a notable 200-fold preference for FKBP52 over FKBP12.

SAFit1 is an inhibitor of FK506 binding protein 51 (FKBP51)-specific (Ki: 4±0.3 nM).

MJC13 is an FKBP52-targeting agent with antitumor activity, suitable for prostate cancer research.

FKBP51F67V-selective antagonist Ligand2 (example 3-3), a potent ligand, selectively binds to FKBP51 F67V variant without affinity for wild-type FKBP51 or FKBP52 [1], and effectively reverses the anxiogenic phenotype resulting from FKBP51 F67V overexpression in the amygdala.

FKBP51-Hsp90-IN-2 (Compound E08) functions as a selective inhibitor for the FKBP51 - Hsp90 protein-protein interaction, exhibiting IC 50 values of 0.4 µM for FKBP51 and 5 µM for FKBP52. Beyond its inhibitory actions, FKBP51-Hsp90-IN-2 enhances cellular energy metabolism and promotes neurite growth. This compound is utilized in the study of neurodegenerative diseases and cancer [1].