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FKBP

The FKBPs, or FK506 binding proteins, constitute a family of proteins that have prolyl isomerase activity and are related to the cyclophilins in function, though not in amino acid sequence. FKBPs have been identified in many eukaryotes, ranging from yeast to humans, and function as protein folding chaperones for proteins containing proline residues. Along with cyclophilin, FKBPs belong to the immunophilin family.

Rapamycin
T153753123-88-9
Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.
  • $30
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Shield-1
T13884914805-33-7
Shield-1 is a specific, high-affinity, and cell-permeable ligand for FK506-binding protein 12 (FKBP) and reverses instability by binding to mutant FKBP (mtFKBP), allowing conditional expression of mtFKBP fusion proteins.
  • $163
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SAFit2
T168361643125-33-0In house
SAFit2 is a highly potent and selective inhibitor of fk506 binding protein 51 (FKBP51) with a Ki value of 6 nM. SAFit2 can enhance the binding of AKT2-AS160 and participate in the downstream response of glucocorticoid release in vivo. It is a candidate compound for the treatment of obesity, chronic pain, depression and anxiety.
  • $84
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AP20187
T14299195514-80-8
AP20187 (B B Homodimerizer) is a cell-permeable compound used to dimerize FK506-binding protein (FKBP) fusion proteins, thereby initiating biological signaling cascades, gene expression, or disrupting protein-protein interactions.
  • $94
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Everolimus
T1784159351-69-6
Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.
  • $37
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Rimiducid
T14298195514-63-7
Rimiducid is a lipid-permeable tacrolimus analogue, homodimerizing an analogue of human protein fkbp12 and binding to wild-type fkbp12 with 1000-fold lower affinity. Rimiducid is a dimerizer agent that acts by cross-linking the FKBP domains. It dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.
  • $138
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SLF-amido-C2-COOH
T139141092369-24-8
SLF-amido-C2-COOH (ZZY01-083) is an FKBP ligand with potential antimicrobial activity for the synthesis of PROTAC.
  • $48
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FKBP12 PROTAC dTAG-13
T112912064175-41-1
FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.
  • $74
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ElteN378
T99501421366-99-5
ElteN378 is a highly potent synthetic inhibitor of FKBP12 with Ki of 0.5 nM, a low atomic weight ligand with affinity comparable to that of the macrolide Rapamycin.
  • $179
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FKBP12 PROTAC RC32
T136942375555-66-9
FKBP12 PROTAC RC32 is a PROTAC-like degrader targeting FKBP12. It can degrade FKBP12 in organs after intraperitoneal administration.
  • $215
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Etonogestrel
T256754048-10-1
Etonogestrel (Implanon) is a steroidal progestin used as hormonal contraceptives.
  • $32
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Ascomycin
T2481104987-12-4
Ascomycin (Immunomycin)(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.
  • $36
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Tacrolimus monohydrate
T20879109581-93-3
Tacrolimus monohydrate (LCP-Tacro) is a macrolide from the culture broth of a strain of Streptomyces tsukubaensis, 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. It prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro and has strong immunosuppressive activity in vivo.
  • $39
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GPI-1046
T11451186452-09-5
GPI-1046 is an immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core.
  • $52
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SLF
T13888195513-96-3
SLF is a synthetic ligand for FKBP12, which increases Ca2+ efflux and protein synthesis to improve skeletal muscle function, and is used in the study of central nervous system diseases and cancer.
  • $99
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ILS-920
T13734892494-07-4
ILS-920 is a Rapamycin analog characterized by diminished immunosuppressive effects but remarkable neuroprotective properties. It exhibits selective binding affinity towards the immunophilin FKBP52 as well as the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 displays a notable 200-fold preference for FKBP52 over FKBP12.
  • $1,520
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FKBP12 PROTAC dTAG-7
T112922064175-32-0In house
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.
  • $1,850
35 days
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AP1867-3-(aminoethoxy)
T135492127390-15-0In house
AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.
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    PROTAC FKBP Degrader-3
    T186102079056-43-0
    PROTAC FKBP Degrader-3 is a potent FKBP degrader, consisting of a FKBP ligand binding group, a linker, and a VHL binding group [1].
    • $493
    10-14 weeks
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    FKBP12 Ligand-Linker Conjugate 1
    T2054362765059-01-4
    FKBP12 Ligand-Linker Conjugate 1 is a complex comprising a target protein ligand for FKBP12 and a linker, which is utilized in the synthesis of the PROTAC degrader MC-25B.
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    SKF1
    T28790678997-25-6
    SKF1 is a suppressor of the ability of FK506. SKF1 inhibits cell growth in the presence of high levels of NaCl, induces cell death in low salt conditions, interacts directly with yeast mitochodria.
    • $1,520
    6-8 weeks
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    SLF TFA
    T738172378802-47-0
    SLF TFA, a synthetic ligand for FK506-binding protein (FKBP), exhibits affinity toward FKBP51 with a value of 3.1 μM and demonstrates an IC50 of 2.6 μM for FKBP12. This compound is utilized in the synthesis of PROTAC [1] [2] [3].
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    Everolimus-d4
    TMIH-02271338452-54-2
    Everolimus-d4 is a deuterated compound of Everolimus.
    • Preferential
    7-10 days
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    MJC13
    T204886200709-97-3
    MJC13 is an FKBP52-targeting agent with antitumor activity, suitable for prostate cancer research.
    • Inquiry Price
    10-14 weeks
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