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-114434
    AP1867
    		99.48%
    AP1867 is a synthetic FKBP12F36V-directed ligand.
    AP1867
  • HY-145514D
    dTAGV-1
    		Degrader 98.43%
    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-114420
    AP1867-2-(carboxymethoxy)
    		Inhibitor 99.88%
    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)
  • HY-130835
    FKBP12 PROTAC RC32
    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-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-103634
    dFKBP-1
    		Inhibitor 98.00%
    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-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-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-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-B0652
    Etonogestrel
    		Agonist 99.91%
    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-10219G
    Rapamycin (GMP)
    Rapamycin (Sirolimus) (GMP) is Rapamycin (HY-10219) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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 (GMP)
  • 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
    		99.14%
    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-163807
    22-SLF
    		Degrader
    22-SLF is a PROTAC degrader, that degrades FK506-binding protein 12 (FKBP12) with a DC50 of 0.5 µM. 22-SLF interacts with C227 and C228 in FBXO22 to induce a ternary complex between FKBP12 and FBXO22, and degrades FKBP12 in a FBXO22-dependent manner. 22-SLF can be used for fundamental cancer research as a probe to study the FBXO22 degradation pathway. (Pink: FKBP12 ligand (HY-114872); Black: Linker (HY-163821); Blue: FBXO22 ligand (HY-163826)).
    22-SLF
  • HY-P4581
    Suc-Ala-Leu-Pro-Phe-pNA
    		Substrate 99.41%
    Suc-Ala-Leu-Pro-Phe-pNA (Suc-ALPF-pNA) is a synthetic polypeptide substrate that targets FK506-binding protein (FKBP). Suc-Ala-Leu-Pro-Phe-pNA can be used to determine peptidyl-prolyl cis-trans isomerase activity via the chymotrypsin-coupled assay. Suc-Ala-Leu-Pro-Phe-pNA serves as a substrate for human FK506-binding protein hFKBP-12 in the chymotrypsin-FKBP coupled PPIase assay. Suc-Ala-Leu-Pro-Phe-pNA is applicable for the detection and research of PPIase activity.
    Suc-Ala-Leu-Pro-Phe-pNA
  • 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-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.
    SP3N hydrochloride
  • 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>
Cat. No. Product Name / Synonyms Application Reactivity