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-153806
    RapaBlock
    		Modulator ≥98.0%
    RapaBlock is a potent, non-immunosuppressive and brain-impermeable FKBP12 ligand.
    RapaBlock
  • HY-107452
    SLF-amido-C2-COOH
    		99.63%
    SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) is a synthetic ligand for FKBP (SLF). SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) can be used in the synthesis of PROTACs.
    SLF-amido-C2-COOH
  • 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-10219R
    Rapamycin (Standard)
    Rapamycin (Standard) is the analytical standard of Rapamycin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-102079
    SAFit1
    		Inhibitor 99.49%
    SAFit1 is a FK506 binding protein 51 (FKBP51)-specific inhibitor with a Ki of 4±0.3 nM.
    SAFit1
  • 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-129610
    KB02-SLF
    		Inhibitor 99.25%
    KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF.
    KB02-SLF
  • HY-135345
    PROTAC FKBP Degrader-3
    		99.48%
    PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader.
    PROTAC FKBP Degrader-3
  • HY-129363
    AP1867-3-(aminoethoxy)
    		98.60%
    AP1867-3-(aminoethoxy), the AP1867 based moiety, is a synthetic ligand for FKBP. AP1867-3-(aminoethoxy) can be used in the synthesis of PROTAC FKBP12 F36V degrader.
    AP1867-3-(aminoethoxy)
  • HY-145514A
    dTAGV-1-NEG
    		99.73%
    dTAGV-1-NEG is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1 is an FKBP12F36V-selective degrader.
    dTAGV-1-NEG
  • 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.
    Rapamycin-d<sub>3</sub>
  • HY-126316
    Zapalog
    		Modulator 98.16%
    Zapalog is a photocleavable small-molecule heterodimerizer that can be used to repeatedly initiate, and instantaneously terminate, a physical interaction between two target proteins. Zapalog dimerizes any two proteins tagged with the FKBP and DHFR domains until exposure to light causes its photolysis.
    Zapalog
  • HY-136424
    GPI-1485
    		99.88%
    GPI-1485 (GM1485), a nonimmunosuppressive immunophilin ligand, promotes neurofunctional improvement and neural regeneration following stroke.
    GPI-1485
  • HY-13756S
    Tacrolimus-13C,d2
    		98.36%
    Tacrolimus-13C,d2 is a 13C-labeled and 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.
    Tacrolimus-<sup>13</sup>C,d<sub>2</sub>
  • HY-P4581
    Suc-Ala-Leu-Pro-Phe-pNA
    		99.80%
    Suc-Ala-Leu-Pro-Phe-pNA (Suc-ALPF-pNA) is a substrate of FK-506 binding protein (FKBP).
    Suc-Ala-Leu-Pro-Phe-pNA
  • HY-145712
    ElteN378
    		Inhibitor 99.96%
    ElteN378 is an inhibitors of FKBP12e. ElteN378 can be used in study Alzheimer disease, Parkinson disease, Amyotrophic Lateral Sclerosis, proliferation disorders and cancer.
    ElteN378
  • 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. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs).
    Etonogestrel
  • 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)).
    22-SLF
  • 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-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>
Cat. No. Product Name / Synonyms Application Reactivity