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-161794
    SP3N
    		Degrader
    SP3N is a specific degrader of the prolyl isomerase FKBP12. The alkylamine of SP3N is metabolized to a reactive aldehyde (SP3CHO), which recruits the SCFFBXO22 ligase for FKBP12 degradation. SP3N may be used in research for cancer.
    SP3N
  • 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-10218S
    Everolimus-d4
    		98.74%
    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.
    Everolimus-d<sub>4</sub>
  • HY-170987
    FKBP12 Ligand-Linker Conjugate 1
    		Ligand
    FKBP12 Ligand-Linker Conjugate 1 is the conjugate composed of a target protein ligand for FKBP12 and a linker. FKBP12 Ligand-Linker Conjugate 1 can be used for synthesis of PROTAC degrader MC-25B (HY-170983).
    FKBP12 Ligand-Linker Conjugate 1
  • HY-114872A
    SLF TFA
    		99.58%
    SLF TFA is a synthetic ligand for FK506-binding protein (FKBP) with an affinity of 3.1 μM for FKBP51 and an IC50 of 2.6 μM for FKBP12. SLF TFA can be used in the synthesis of PROTAC.
    SLF TFA
  • 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-13557R
    Ascomycin (Standard)
    		Inhibitor
    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].
    Ascomycin (Standard)
  • 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-173082
    10-SLF
    		Degrader
    10-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. Pink: FKBP12 ligand (HY-170988); Black: linker (HY-W004640); Blue: E3 ligase ligand.
    10-SLF
  • HY-176502
    FKBP12 ligand-3
    FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 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-3 can be used for selective cancer research based on differences in intracellular presenter protein levels.
    FKBP12 ligand-3
  • 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-145514D
    dTAGV-1
    		Degrader
    dTAGV-1 is a potent and selective degrader of FKBP12F36V-tagged proteins PROTAC degrader. dTAGV-1 can induce degradation of FKBP12F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A)).
    dTAGV-1
  • 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-176477
    BRD4/FKBP12 degrader-2
    		Degrader
    BRD4/FKBP12 degrader-2 (a1dj) is a BRD4/FKBP12 degrader and shows anticancer activity (BRD4 ligand: HY-78695, FKBP12 ligand: HY-176502, linker: HY-140212).
    BRD4/FKBP12 degrader-2
  • 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. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs).
    Etonogestrel-d<sub>6</sub>
Cat. No. Product Name / Synonyms Application Reactivity