fkbp5

UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy.

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-1 (Compound D10) serves as a selective inhibitor targeting the FKBP51-Hsp90 protein-protein interaction, demonstrating an IC 50 value of 0.1 μM against FKBP51. It holds potential for research applications in stress-related diseases, Alzheimer's disease, and metabolic disorders [1].

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].

SAFit2 is a highly potent and selective inhibitor of fk506 binding protein 51 (FKBP51) with a Ki value of 6 nM. SAFit2 can enhance the binding of AKT2-AS160 and participate in the downstream response of glucocorticoid release in vivo. It is a candidate compound for the treatment of obesity, chronic pain, depression and anxiety.

Etonogestrel (Implanon) is a steroidal progestin used as hormonal contraceptives.

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.

SLF is a synthetic ligand for FKBP12, which increases Ca2+ efflux and protein synthesis to improve skeletal muscle function, and is used in the study of central nervous system diseases and cancer.

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