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

FKBP

FKBP

Related Products

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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.

FKBP Related Products (67):

Cat. No. Product Name Effect Purity
  • HY-13756
    Tacrolimus
    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[1].
  • HY-10218
    Everolimus
    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[1][2].
  • HY-13992
    AP20187 Modulator
    AP20187 (B/B Homodimerizer) is a cell-permeable ligand used to dimerize FK506-binding protein (FKBP) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.
  • HY-114421
    FKBP12 PROTAC dTAG-13 Degrader 99.89%
    FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12F36V and CRBN, thereby selectively degrading FKBP12F36V[1].
  • HY-10219
    Rapamycin
    Rapamycin (Sirolimus; AY 22989) 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[1]. Rapamycin is an autophagy activator, an immunosuppressant[2].
  • HY-161794A
    SP3N hydrochloride Degrader 99.84%
    SP3N hydrochloride is a specific degrader of the prolyl isomerase (FKBP12). The alkylamine of SP3N hydrochloride is metabolized to a reactive aldehyde (SP3CHO), which recruits the SCFFBXO22 ligase for FKBP12 degradation. SP3N hydrochloride may be used in research for cancer[1].
  • HY-13756S2
    Tacrolimus-d3
    Tacrolimus-d3 (FK506-d3) is deuterium labeled Tacrolimus. 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[1].
  • HY-10218S1
    Everolimus-13C2,d4
    Everolimus-13C2,d4 (RAD001-13C2,d4) is 13C labeled Everolimus. 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[1][2].
  • HY-16046
    Rimiducid Activator 99.81%
    Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains. Rimiducid (AP1903) dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.
  • 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)[1].
  • HY-163807
    22-SLF Degrader
    22-SLF is a PROTAC degrader, that degrades FK506-binding protein 12 (FKBP12) with a DC50 of 0.5 µM in a FBXO22 dependent manner. 22-SLF degrades other endogenous proteins, such as BRD4 and EML4-ALK fusion protein.(Pink: Ligand for target protein SLF (HY-114872); Black: Linker (HY-163821); Blue: Ligand for E3 ligase (HY-163826))[1].
  • 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[1].
  • HY-10219S
    Rapamycin-d3
    Rapamycin-d3 is the deuterium labeled Rapamycin. 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[1][2].
  • 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].
  • HY-114434
    AP1867 99.43%
    AP1867 is a synthetic FKBP12F36V-directed ligand[1].
  • 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[1].
  • HY-13557
    Ascomycin Inhibitor
    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].
  • HY-B0652
    Etonogestrel Agonist 99.14%
    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].
  • 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[1][2].
  • 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[1].