FKBP
FK506-binding protein
FKBPs (FK506-binding proteins) belong to a distinct class of immunophilins that interact with immunosuppressants, such as FK506 and Rapamycin. FKBPs use their peptidyl-prolyl isomerase (PPIase) activity to catalyze the cis-trans conversion of prolyl bonds in proteins during protein-folding events. FKBPs also act as a unique group of chaperones. FKBPs are involved in several biochemical processes including protein folding, receptor signaling, protein trafficking and transcription. FKBP family proteins play important functional roles in the T-cell activation, when complexed with their ligands.
FKBPs, through interactions with steroid hormone receptors, kinases, or other cellular factors, play important roles in various physiological processes and, more interestingly, in pathological processes in mammals. Mammalian FKBPs can be divided into four groups: cytoplasmic, TPR domain, endoplasmic reticulum (ER) or secretory pathway and nuclear. The cytoplasmic FKBP isoforms FKBP12 and 12.6 and the nuclear FKBP25 and 133 contain a single PPIase domain. FKBP36, 38, 51 and 52 contain multiple TPR domains. The ER FKBPs: FKBP13, 19, 22, 23, 60 and 65 all contain an N-terminal ER signal peptide.
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FKBP Inhibitors
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FKBP Agonists
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FKBP Antagonist
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FKBP Activator
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FKBP Modulators
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FKBP Degraders
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FKBP Controls
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FKBP Substrate
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FKBP Ligands
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FKBP Verwandte Produkte (86)
Verwandte Produkte (86)
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Antibodies (5)
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Everolimus-d4
0 ImagesSynonyms: RAD001-d4; SDZ-RAD-d4Everolimus-d4 is the deuterium labeled Everolimus. Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.
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Rapamycin (GMP Like)
0 ImagesSynonyms: Sirolimus (GMP Like); AY-22989 (GMP Like); NSC 226080 (GMP Like)Rapamycin (Sirolimus) GMP Like is Rapamycin (HY-10219) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
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Zapalog
0 ImagesZapalog is a photocleavable small-molecule heterodimerizer that can be used to repeatedly initiate, and instantaneously terminate, a physical interaction between two target proteins. Zapalog dimerizes any two proteins tagged with the FKBP and DHFR domains until exposure to light causes its photolysis.
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GPI-1485
0 ImagesSynonyms: GM1485GPI-1485 (GM1485), a nonimmunosuppressive immunophilin ligand, promotes neurofunctional improvement and neural regeneration following stroke.
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Rapamycin-13C,d3
0 ImagesArt. -Nr.: HY-10219S1Synonyms: Sirolimus-13C,d3; AY-22989-13C,d3 NSC 226080-13C,d3Rapamycin-13C,d3 (Sirolimus-13C,d3) is the 13C, deuterated-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
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Ascomycin (Standard)
0 ImagesSynonyms: Immunomycin (Standard); FR-900520 (Standard); FK520 (Standard)Ascomycin (Standard) is the analytical standard of Ascomycin. This product is intended for research and analytical applications. Ascomycin (Immunomycin; FR-900520; FK520) is an ethyl analog of Tacrolimus (FK506) with strong immunosuppressant properties. Ascomycin is also a macrocyclic polyketide antibiotic with multiple biological activities such as anti-malarial, anti-fungal and anti-spasmodic. Ascomycin prevents graft rejection and has potential for varying skin ailments research[1][2].
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WAY-380153
0 ImagesWAY-380153 (Compound 24) is an FKBP12 inhibitor. WAY-380153 exhibits moderate binding affinity for FKBP12, with a KD of 19 μM (measured by ITC) and 15 μM (measured by NMR). WAY-380153 can be used in research related to neurotrophy and neuroprotection.
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ILS-920
0 ImagesILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 shows 200-fold selectivity for FKBP52 versus FKBP12.
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Tacrolimus-d3
0 ImagesArt. -Nr.: HY-13756S2Synonyms: FK506-d3; Fujimycin-d3; FR900506-d3Tacrolimus-d3 (FK506-d3) is the deuterated-labeled Tacrolimus (HY-13756). Tacrolimus (FK506), a molecular glue, a macrocyclic lactone, 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.
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FKBP12 ligand-2
0 ImagesArt. -Nr.: HY-176501CAS. Nr.: 3036243-81-6FKBP12 ligand-2 (compound d) is a high affinity ligand targeting FKBP12. FKBP12 ligand-2 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-2 can be used for selective cancer research based on differences in intracellular presenter protein levels.
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FKBP51F67V-selective antagonist Ligand2
0 ImagesArt. -Nr.: HY-153990CAS. Nr.: 1680228-76-5FKBP51F67V-selective antagonist Ligand2 (example 3-3) is a potent FKBP51 F67V-selective antagonist ligand. FKBP51F67V-selective antagonist Ligand2 reverses the anxiogenic phenotype induced by overexpression of FKBP51 F67V in the amygdala. FKBP51F67V-selective antagonist Ligand2 binds to FKBP51 F67V, but not to wild-type FKBP51 or FKBP52.
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dTAGV-1-NEG TFA
0 ImagesArt. -Nr.: HY-145514BdTAGV-1-NEG TFA is an inactive FKBP12F36V PROTAC degrader, the diastereomer of dTAGV-1 (HY-145514D), and a heterobifunctional negative control molecule. dTAGV-1-NEG TFA does not degrade any protein.
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FKBP51-Hsp90-IN-1
0 ImagesArt. -Nr.: HY-158130CAS. Nr.: 433313-64-5FKBP51-Hsp90-IN-1 (Compound D10) is a selective inhibitor of the FKBP51-Hsp90 protein-protein interaction, with an IC50 value of 0.1 μM against FKBP51. FKBP51-Hsp90-IN-1 can be used in the research of stress-related diseases, Alzheimer's disease, and metabolic disorders.
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10-SLF
0 ImagesArt. -Nr.: HY-173082CAS. Nr.: 2765058-89-510-SLF is a PROTAC FKBP12 degrader. 10-SLF induces a ternary complex between FKBP12 and FBXW7-R465C, and promotes FBXW7-R465C-dependent proteasomal degradation of FKBP12. 10-SLF selectively reduces FKBP12 levels in cells expressing FBXW7-R465C.
