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-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-10219S1
    Rapamycin-13C,d3
    Rapamycin-13C,d3 (Sirolimus-13C,d3; AY-22989-13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219).Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
    Rapamycin-<sup>13</sup>C,d<sub>3</sub>
  • HY-10218S
    Everolimus-d4
    Everolimus-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[1][2].
    Everolimus-d<sub>4</sub>
  • 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-169148
    YT117R
    		Degrader
    YT117R is a PROTAC degrader of FKBP12 and Pink: Target protein ligand: (HY-158301); Black: linker (HY-42776); Blue: E3 ligase ligand (HY-78695)).
    YT117R
  • 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-170988
    FKBP12 ligand-1
    		Ligand
    FKBP12 ligand-1 is a targeting protein ligand of MC-25B (HY-170983), which is a specific FKBP12 PROTAC.
    FKBP12 ligand-1
  • HY-B0652R
    Etonogestrel (Standard)
    		Agonist
    Etonogestrel (Standard) is the analytical standard of Etonogestrel. This product is intended for research and analytical applications. Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs).
    Etonogestrel (Standard)
  • HY-B0652S1
    Etonogestrel-d6
    		Agonist
    Etonogestrel-d6 is deuterium labeled Etonogestrel. Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs[1]. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs)[2].
    Etonogestrel-d<sub>6</sub>
  • 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-170983
    MC-25B
    		Inhibitor
    MC-25B is a specific FKBP12 PROTAC degrader. MC-25B degrades FKBP12 with a DC50 of 0.35 μM and a Dmax of 89%. MC-25B facilitates the degradation of nuclear-localized FKBP12 through a DCAF16-dependent mechanism. (Pink: FKBP12 ligand (HY-170988); Blue: E3 ligase ligand HY-170986); Black: linker (HY-128844); FKBP12 ligand+ linker (HY-170987)).
    MC-25B
  • 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-129664
    L 683519
    		Inhibitor
    L 683519, one of the impurities of tacrolimus, is an immunosuppressant. L 683519 can inhibit the activity of FK-506 binding protein.
    L 683519
  • 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-172152
    MP-010
    		Ligand
    MP-010 is a FKBP12 ligand that regulates cytosolic calcium by stabilizing RyR channel activity. MP-010 promotes functional improvement in SOD1G93A amyotrophic lateral sclerosis (ALS) mice, as evidenced by improved motor coordination, increased integrity of neuromuscular junctions, and significantly enhanced survival of spinal motor neurons. MP-010 can be used for research in the field of neurological diseases.
    MP-010
  • 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)
Cat. No. Product Name / Synonyms Application Reactivity