FKBP

FK506-binding protein

FKBP

Related Products

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.

FKBP Related Products (50)
Antibodies (5)

By Effects:	Inhibitors (13) Agonists (2) Degraders (5) Antagonist (1) Activator (1) Modulators (5)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-102079

SAFit1	Inhibitor	99.71%
SAFit1 is a FK506 binding protein 51 (FKBP51)-specific inhibitor with a K_i of 4±0.3 nM.

HY-153806

RapaBlock	Modulator	≥98.0%
RapaBlock is a potent, non-immunosuppressive and brain-impermeable FKBP12 ligand.

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.

HY-147098

dTAG-47	Inhibitor	99.65%
dTAG-47, heterobifunctional dTAG molecule, targets mutant FKBP12 (FKBP12^F36V). FKBP12^F36V serves as a degradation tag (dTAG) and is fused to a protein of interest. dTAG-47 can be used for the research of basal-like breast cancers (BBC).

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.

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.

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.

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[1].

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.

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.

HY-145514C

dTAGV-1 hydrochloride	Degrader	98.83%
dTAGV-1 hydrochloride is the hydrochloride form of dTAGV-1 that is a small molecule degrader of FKBP12.

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.

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).

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).

HY-114872A

SLF TFA		99.58%
SLF TFA 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 TFA can be used in the synthesis of PROTAC.

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.

HY-145514A

dTAGV-1-NEG
dTAGV-1-NEG is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1 is an FKBP12^F36V-selective degrader.

HY-10218S

Everolimus-d₄
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[1][2].

HY-153990

FKBP51F67V-selective antagonist Ligand2	Antagonist
FKBP51F67V-selective antagonist Ligand2 (example 3-3) is a potent FKBP51 F67V-selective antagonist ligand. FKBP51F67V-selective antagonist Ligand2 reverses the anxiogenic phenotype induced by overexpression of FKBP51 F67V in the amygdala. FKBP51F67V-selective antagonist Ligand2 binds to FKBP51 F67V, but not to wild-type FKBP51 or FKBP52.

HY-145514B

dTAGV-1-NEG TFA
dTAGV-1-NEG TFA is a diastereomer and as a heterobifunctional negative control of dTAGV-1. dTAGV-1-NEG TFA is an FKBP12^F36V-selective degrader.

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FKBP

FKBP

FKBP Related Products (50)

Antibodies (5)

FKBP Related Products (50):