fk506-binding protein

Shield-1 is a specific, high-affinity, and cell-permeable ligand for FK506-binding protein 12 (FKBP) and reverses instability by binding to mutant FKBP (mtFKBP), allowing conditional expression of mtFKBP fusion proteins.

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

Tacrolimus monohydrate (LCP-Tacro) is a macrolide from the culture broth of a strain of Streptomyces tsukubaensis, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties. It prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro and has strong immunosuppressive activity in vivo.

Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

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

GPI-1046 is an immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core.

Rimiducid is a lipid-permeable tacrolimus analogue, homodimerizing an analogue of human protein fkbp12 and binding to wild-type fkbp12 with 1000-fold lower affinity. Rimiducid is a dimerizer agent that acts by cross-linking the FKBP domains. It dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.

AP20187 (B/B Homodimerizer) is a cell-permeable compound used to dimerize FK506-binding protein (FKBP) fusion proteins, thereby initiating biological signaling cascades, gene expression, or disrupting protein-protein interactions.

Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.

Ascomycin (Immunomycin)(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.

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.

AP1867 (FK506-binding protein) is a synthetic FKBP12 F36V-directed ligand attached to 320 substituted tetrahydrooxazepines (THOXs). AP1867 (FK506-binding protein) was synthesized via combined liquid- and solid-phase methods employing sequential Mitsunobu displacements followed by ruthenium-mediated olefin metathesis to close seven-membered rings; the resin-bound THOX ligands were coupled to AP1867 in parallel, yielding candidate heterodimerizers that demonstrated membrane permeability and bioactivity in human fibrosarcoma cells, facilitating the study of targeted protein interactions and intracellular modulation.

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.

Supradamal is a potent Inhibitor of Plasmodium FK506 Binding Protein 35 (FKBD35). It also acts as an HIV inhibitor.

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].

22-SLF is a PROTAC degrader that operates by FBXO22-dependent degradation of FK506 Binding Protein 12 (FKBP12) with a DC50 of 0.5 µM. Additionally, 22-SLF can degrade other endogenous proteins, such as BRD4 and the EML4-ALK fusion protein (EML4-ALK fusion protein).

FKBPL (FK506-binding protein like)-based peptide. Binds to and upregulates expression of CD44. Inhibits breast cancer stem cell (BCSC) growth. Decreases pluripotency markers and promotes differentiation of BCSCs. Also inhibits endothelial cell migration a