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-170983
    MC-25B
    		Inhibitor
    MC-25B is a specific FKBP12 PROTAC degrader. MC-25B degrades FKBP12 with a DC50 of 0.35 μM and a Dmax of 89%. MC-25B facilitates the degradation of nuclear-localized FKBP12 through a DCAF16-dependent mechanism. (Pink: FKBP12 ligand (HY-170988); Blue: E3 ligase ligand HY-170986); Black: linker (HY-128844); FKBP12 ligand+ linker (HY-170987)).
    MC-25B
  • HY-106345
    ILS-920
    ILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 shows 200-fold selectivity for FKBP52 versus FKBP12.
    ILS-920
  • HY-147196
    KB03-SLF
    		Degrader
    KB03-SLF (compound 6) is an electrophilic PROTAC degrader that binds to DCAF16 to degrade the nuclear protein FKBP12. KB03-SLF can be used in cancer research. (Pink: Ligand for target protein SLF (HY-114872); Black: Linker (HY-W040168); Blue: Ligand for E3 ligase (HY-169968)).
    KB03-SLF
  • HY-129664
    L 683519
    		Inhibitor
    L 683519, one of the impurities of tacrolimus, is an immunosuppressant. L 683519 can inhibit the activity of FK-506 binding protein.
    L 683519
  • HY-W765245
    Rapamycin-13C,d3-1
    Rapamycin-13C,d3-1 (Sirolimus-13C,d3-1) is the deuterium labeled and 13C-labeled Rapamycin (HY-10219). 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-<sup>13</sup>C,d<sub>3</sub>-1
  • 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-172152
    MP-010
    		Ligand
    MP-010 is a FKBP12 ligand that regulates cytosolic calcium by stabilizing RyR channel activity. MP-010 promotes functional improvement in SOD1G93A amyotrophic lateral sclerosis (ALS) mice, as evidenced by improved motor coordination, increased integrity of neuromuscular junctions, and significantly enhanced survival of spinal motor neurons. MP-010 can be used for research in the field of neurological diseases.
    MP-010
  • 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.
    D44
  • 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.
    Tacrolimus-d<sub>3</sub>
  • 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.
    Everolimus-<sup>13</sup>C<sub>2</sub>,d<sub>4</sub>
  • HY-W520748
    MJC13
    MJC13 is an FKBP52-targeted agent with anti-tumor activity that can be used in prostate cancer research.
    MJC13
  • HY-113646
    Shield-2
    		Modulator
    Shield-2 is an efficient stabilizing ligand binding to the FKBP (F36V) protein with a dissociation constant of 29 nM. Shield-2 binds tightly to the FKBP mutants destabilizing domains and prevents degradation, thus providing small molecule regulation over intracellular protein levels.
    Shield-2
Cat. No. Product Name / Synonyms Application Reactivity