fkbp51

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.

SAFit1 is a highly potent and selective inhibitor of FK506 binding protein 51 (FKBP51) with a Ki value of 4 ± 0.3 nM, extensively applied in stress biology, neuropsychiatric disorder research, and metabolic disease studies to dissect FKBP51-specific signaling pathways and evaluate its role as a therapeutic target distinct from closely related FKBP family members.

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].

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.

SLF TFA, a synthetic ligand for FK506-binding protein (FKBP), exhibits affinity toward FKBP51 with a value of 3.1 μM and demonstrates an IC50 of 2.6 μM for FKBP12. This compound is utilized in the synthesis of PROTAC [1] [2] [3].