2. Signaling Pathways
  3. Apoptosis
    Autophagy
    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-10219
    Rapamycin
    		99.94%
    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. Rapamycin is an autophagy activator, an immunosuppressant.
    Rapamycin
  • HY-10218
    Everolimus
    		99.68%
    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
  • HY-13756
    Tacrolimus
    		99.93%
    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
  • HY-112210
    Shield-1
    		Modulator 99.52%
    Shield-1 (Shld1) is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize proteins tagged with a mutated FKBP12-derived destabilization domain (DD).
    Shield-1
  • 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.
    Rimiducid
  • 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-145514C
    dTAGV-1 hydrochloride
    		Degrader
    dTAGV-1 hydrochloride is the hydrochloride form of dTAGV-1 that is a small molecule degrader of FKBP12.
    dTAGV-1 hydrochloride
  • 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-13992
    AP20187
    		Modulator 99.88%
    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.
    AP20187
  • HY-114421
    FKBP12 PROTAC dTAG-13
    		Degrader 99.75%
    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.
    FKBP12 PROTAC dTAG-13
  • HY-102080
    SAFit2
    		Inhibitor 98.59%
    SAFit2 is a highly potent, highly selective FK506-binding protein 51 (FKBP51) inhibitor with a Ki of 6 nM and also enhances AKT2-AS160 binding.
    SAFit2
  • HY-13756A
    Tacrolimus monohydrate
    		99.67%
    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
  • HY-114434
    AP1867
    		99.43%
    AP1867 is a synthetic FKBP12F36V-directed ligand.
    AP1867
  • HY-13557
    Ascomycin
    		Inhibitor ≥98.0%
    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.
    Ascomycin
  • HY-114872
    SLF
    		98.60%
    SLF 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 can be used in the synthesis of PROTAC.
    SLF
  • HY-123941
    FKBP12 PROTAC dTAG-7
    		Inhibitor 99.88%
    FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.
    FKBP12 PROTAC dTAG-7
  • HY-130835
    FKBP12 PROTAC RC32
    		98.58%
    FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin (HY-10219) and a ligand for an Cereblon E3 ubiquitin ligase (Pomalidomide; HY-10984).
    FKBP12 PROTAC RC32
  • HY-124619
    GPI-1046
    		99.74%
    GPI-1046 is a immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models. GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models. GPI-1046 improves HIV-associated injury of peripheral nerves.
    GPI-1046
  • HY-103634
    dFKBP-1
    		Inhibitor
    dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF (HY-114872) of FKBP12, the Thalidomide based Cereblon ligand and a linker.
    dFKBP-1
  • HY-114420
    AP1867-2-(carboxymethoxy)
    		Inhibitor 99.85%
    AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules.
    AP1867-2-(carboxymethoxy)
Cat. No. Product Name / Synonyms Application Reactivity