fk 506

(E/Z)-FK-506 26,28-Allylic ester rearrangement impurity (FK506-A) is an impurity found in Tacrolimus.

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.

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.

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.

Tacrolimus-BSA is a hapten-carrier protein conjugate formed by coupling Tacrolimus to bovine serum albumin (BSA). As a hapten, Tacrolimus alone cannot induce an immune response and must be conjugated to a large molecular protein to become a complete antigen with immunogenicity. Tacrolimus-BSA may be supplied as a lyophilized powder or as a solution. The solution is prepared in 0.01 M TBS (pH 7.4) buffer at a typical concentration of 1 mg/mL.

13-O-Desmethyl tacrolimus (13-DMT; 13-O-Demethyl FK 506) is the primary metabolite of Tacrolimus. It exhibits weaker immunosuppressive activity compared to Tacrolimus. This compound is primarily utilized in monitoring studies of Tacrolimus through the analysis of the 13-DMT/Tacrolimus ratio.

L 683519 is one of the Tacrolimus impurities with immunosuppressant and could restrain the activity of FK-506 binding protein.

L 685818 is the C18-hydroxy, C21-ethyl of FK-506 analog.

Suc-Ala-Leu-Pro-Phe-pNA (Suc-ALPF-pNA), a substrate for FK-506 binding protein (FKBP) [1], is utilized to demonstrate the complex interactions essential for targeted biochemical assays.