FKBP
FK506-binding protein
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.
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FKBP Inhibitors
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FKBP Agonists
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FKBP Antagonist
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FKBP Activator
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FKBP Modulators
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FKBP Degraders
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FKBP Controls
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FKBP Substrate
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FKBP Ligands
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FKBP Related Products (86)
Related Products (86)
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Antibodies (5)
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FKBP12 ligand-3
0 ImagesCat. No.: HY-176502CAS No.: 3036374-26-9FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels.
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Setafrastat
0 ImagesCat. No.: HY-109102CAS No.: 1399715-48-0Synonyms: TS-133Setafrastat (Compound 40) is a hair growth stimulator.
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FKBP12 PROTAC FM4
0 ImagesFKBP12 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 FKBP12F36V-tagged SARS1. FKBP12 PROTAC FM4 is applicable to research related to HPV-positive cervical cancer.
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SKF1
0 ImagesCat. No.: HY-123454CAS No.: 678997-25-6SKF1 is a FK506 suppressor, causes a mitochondrially induced death in low salt, concomitant with the release of reactive oxygen species (ROS).
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BRD4/FKBP12 degrader-2
0 ImagesCat. No.: HY-176477BRD4/FKBP12 degrader-2 (a1dj) is a BRD4/FKBP12 degrader and shows anticancer activity (BRD4 ligand: HY-78695, FKBP12 ligand: HY-176502, linker: HY-140212).
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Etonogestrel (Standard)
0 ImagesSynonyms: 3-Oxodesogestrel (Standard); 3-keto-Desogestrel (Standard)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).
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Etonogestrel-d6
0 ImagesCat. No.: HY-B0652S1Synonyms: 3-Oxodesogestrel-d6; 3-keto-Desogestrel-d6Etonogestrel-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).
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MC-25B
0 ImagesCat. No.: HY-170983MC-25B is a DCAF16-recruiting FKBP12 PROTAC degrader with a DC50 of 0.35 μM. MC-25B promotes the formation of a ternary complex with DCAF16 and nuclear-localized FKBP12_NLS, thereby mediating DCAF16-dependent degradation of FKBP12_NLS via the proteasome and Cullin-RING ligase pathway.
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AP1867-3-(aminoethoxy) hydrochloride
0 ImagesCat. No.: HY-129363ACAS No.: 2127390-16-1
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KB03-SLF
0 ImagesCat. No.: HY-147196CAS No.: 2384184-42-1KB03-SLF is a bifunctional PROTAC, formed by conjugating the cysteine-targeting KB03 exploratory fragment with SLF (HY-114872), an FKBP12 ligand that does not support the degradation of FKBP12NLS. KB03-SLF fails to degrade nuclear-localized FKBP12NLS in cells, nor can it mediate the interaction between DCAF16 and FKBP12NLS in a manner similar to KB02-SLF (HY-129610).
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AP21998
0 ImagesCat. No.: HY-179354CAS No.: 292606-90-7AP21998 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.
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RAFKBP12
0 ImagesCat. No.: HY-181498CAS No.: 2375455-59-5RAFKBP12 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.
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L 683519
0 ImagesCat. No.: HY-129664CAS No.: 132172-14-6L 683519, one of the impurities of tacrolimus, is an immunosuppressant. L 683519 can inhibit the activity of FK-506 binding protein.
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Rapamycin-13C,d3-1
0 ImagesCat. No.: HY-W765245Synonyms: Sirolimus-13C,d3-1; AY-22989-13C,d3-1Rapamycin-13C,d3-1 (Sirolimus-13C,d3-1) is the deuterated, 13C-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
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FKBP51-Hsp90-IN-2
0 ImagesCat. No.: HY-158131CAS No.: 601511-07-3FKBP51-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.
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MP-010
0 ImagesCat. No.: HY-172152CAS No.: 3024617-59-9MP-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.
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D44
0 ImagesCat. No.: HY-W046346CAS No.: 826998-10-1D44 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.
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SAFit2 (Standard)
0 ImagesCat. No.: HY-102080RCAS No.: 1643125-33-0
