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 (84)
Antibodies (5)

By Effects:	Inhibitors (19) Agonists (3) Degraders (16) Substrate (1) Ligands (5) Antagonist (1) Activator (1) Modulators (5)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-172265

FKBP12 PROTAC FM4	Degrader	99.95%
FKBP12 PROTAC FM4 is a PROTAC degrader of FKBP12, with a DC50 value of 0.09-0.22 nM. FKBP12 PROTAC FM4 inhibits global protein synthesis, induces apoptosis, and selectively reduces the viability of cervical cancer cells expressing MTH1-E6 and FKBP12^F36V-tagged SARS1. FKBP12 PROTAC FM4 is applicable to research related to HPV-positive cervical cancer.

HY-123454

SKF1	Inhibitor
SKF1 is a FK506 suppressor, causes a mitochondrially induced death in low salt, concomitant with the release of reactive oxygen species (ROS).

HY-170988

FKBP12 ligand-1	Ligand
FKBP12 ligand-1 is a targeting protein ligand of MC-25B (HY-170983), which is a specific FKBP12 PROTAC.

HY-176477

BRD4/FKBP12 degrader-2	Degrader
BRD4/FKBP12 degrader-2 (a1dj) is a BRD4/FKBP12 degrader and shows anticancer activity (BRD4 ligand: HY-78695, FKBP12 ligand: HY-176502, linker: HY-140212).

HY-B0652R

Etonogestrel (Standard)	Agonist
Etonogestrel (Standard) is the analytical standard of Etonogestrel. This product is intended for research and analytical applications. 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-B0652S1

Etonogestrel-d₆	Agonist
Etonogestrel-d₆ is deuterium labeled Etonogestrel. 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-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 D_max 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)).

HY-129363A

AP1867-3-(aminoethoxy) hydrochloride
AP1867-3-(aminoethoxy) hydrochloride, the AP1867 (HY-114434) based moiety, is a synthetic ligand for FKBP. AP1867-3-(aminoethoxy) hydrochloride can be used in the synthesis of PROTAC FKBP12 F36V degrader.

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)).

HY-179354

AP21998	Ligand
AP21998 is a Fv (mutant FKBP) domain-selective ligand that binds to a single FKBPv. AP21998 disrupts FKBP-mediated oligomerization, blocks the proliferation of transformed myeloid progenitors and facilitates their terminal myeloid differentiation. AP21998 disrupts aggregates of CAD-hM1 receptor fusion protein, allowing receptors to exit the ER and enter the plasma membrane. AP21998 can be used for cancer research.

HY-181498

RAFKBP12	Degrader
RAFKBP12 is a FKBP12 CAP-TAC (proteinase complex cap-targeted chimera) degrader. RAFKBP12 demonstrates the feasibility of the CAP-TAC strategy, which enables proteasome-dependent degradation of FKBP12 that is independent of E3 ubiquitin ligases and protein ubiquitination.

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.

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.

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.

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 SOD1^G93A 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.

HY-181500

AP1867-NH-PEG3-acid	Ligand
AP1867-NH-PEG3-acid (Compound S15) is a Target Protein Ligand-Linker Conjugate that contains the FKBP12^F36V ligand AP1867 (HY-114434) and a PROTAC linker, and recruits E3 ligase. JQ-1-Azidopropylamine is available for the synthesis of PROTAC RAFKBP12 (HY-181498).

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.

HY-102080R

SAFit2 (Standard)	Inhibitor
SAFit2 (Standard) is the analytical standard of SAFit2 (HY-102080). This product is intended for research and analytical applications. SAFit2, a chemical probe, is a highly potent, highly selective FK506-binding protein 51 (FKBP51) inhibitor with a K_i of 6 nM and also enhances AKT2-AS160 binding.

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.

HY-107452R

SLF-amido-C2-COOH (Standard)
SLF-amido-C2-COOH (Standard) is the analytical standard of SLF-amido-C2-COOH (HY-107452). This product is intended for research and analytical applications. 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.

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FKBP

FKBP

FKBP Related Products (84)

Antibodies (5)

FKBP Related Products (84):