2. Signaling Pathways
  3. Apoptosis
    Autophagy
    Cell Cycle/DNA Damage
    Immunology/Inflammation
  4. FKBP

FKBP

FK506-binding protein

FKBP

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-153990
    FKBP51F67V-selective antagonist Ligand2
    		Antagonist
    FKBP51F67V-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.
    FKBP51F67V-selective antagonist Ligand2
  • HY-145514B
    dTAGV-1-NEG TFA
    dTAGV-1-NEG TFA is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1-NEG TFA is an FKBP12F36V-selective degrader.
    dTAGV-1-NEG TFA
  • HY-158130
    FKBP51-Hsp90-IN-1
    		Inhibitor
    FKBP51-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.
    FKBP51-Hsp90-IN-1
  • HY-109102
    Setafrastat
    		Inhibitor
    Setafrastat (Compound 40) is a hair growth stimulator.
    Setafrastat
  • HY-123454
    SKF1
    		Inhibitor
    SKF1 is a FK506 suppressor, causes a mitochondrially induced death in low salt, concomitant with the release of reactive oxygen species (ROS).
    SKF1
  • HY-10218R
    Everolimus (Standard)
    Everolimus (Standard) is the analytical standard of Everolimus. This product is intended for research and analytical applications. Everolimus (RAD001) is a Rapamycin (HY-10219) 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.
    Everolimus (Standard)
  • HY-106345
    ILS-920
    ILS-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.
    ILS-920
  • HY-147196
    KB03-SLF
    		Degrader
    KB03-SLF (compound 6) is an electrophilic PROTAC degrader that binds to DCAF16 to degrade the nuclear protein FKBP12. KB03-SLF can be used in cancer research. (Pink: Ligand for target protein SLF (HY-114872); Black: Linker (HY-W040168); Blue: Ligand for E3 ligase (HY-169968)).
    KB03-SLF
  • HY-158131
    FKBP51-Hsp90-IN-2
    		Inhibitor
    FKBP51-Hsp90-IN-2 (Compound E08) is a selective FKBP51-Hsp90 protein-protein interaction inhibitor with IC50 values of 0.4 µM and 5 µM for FKBP51 and FKBP52, respectively. FKBP51-Hsp90-IN-2 also effectively stimulates cellular energy metabolism and neurite growth. FKBP51-Hsp90-IN-2 can be used in research on neurodegenerative diseases and cancer.
    FKBP51-Hsp90-IN-2
  • HY-13756AR
    Tacrolimus (monohydrate) (Standard)
    Tacrolimus (monohydrate) (Standard) is the analytical standard of Tacrolimus (monohydrate). This product is intended for research and analytical applications. Tacrolimus monohydrate (FK506 monohydrate), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex and inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties.
    Tacrolimus (monohydrate) (Standard)
  • HY-13756R
    Tacrolimus (Standard)
    Tacrolimus (Standard) is the analytical standard of Tacrolimus. This product is intended for research and analytical applications. Tacrolimus (FK506), 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.
    Tacrolimus (Standard)
  • HY-W046346
    D44
    		Inhibitor
    D44 is a Plasmodium FKBP35 inhibitor that selectively inhibits the FKBD35 PPIase activity, with PPIase IC50 values of 132 nM and 125 nM for Plasmodium falciparum and Plasmodium vivax, respectively. D44 exhibits antiplasmodium activity and can be used in research related to infectious diseases.
    D44
  • HY-113646
    Shield-2
    		Modulator
    Shield-2 is an efficient stabilizing ligand binding to the FKBP (F36V) protein with a dissociation constant of 29 nM. Shield-2 binds tightly to the FKBP mutants destabilizing domains and prevents degradation, thus providing small molecule regulation over intracellular protein levels.
    Shield-2
Cat. No. Product Name / Synonyms Application Reactivity