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.

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

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