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FKBP

FKBP

FKBPs (FK506-binding proteins) interact with immunosuppressants like FK506 and Rapamycin. They are a special class of immunophilins. During protein folding processes, FKBPs use their peptidyl-prolyl isomerase (PPIase) activity to catalyze the cis-trans conversion of prolyl bonds in proteins. The FKBPs serve as an exceptional group of chaperones. Protein folding, receptor signaling, protein trafficking, and transcription are just a few of the biochemical processes that FKBPs are involved in. When they are complexed with their ligands, proteins from the FKBP family have significant functional roles in the activation of T cells.

Through their interactions with kinases, steroid hormone receptors, and other cellular components, FKBPs contribute significantly to a number of physiological processes and, more intriguingly, to pathological processes in mammals. Four categories—cytoplasmic, TPR domain, endoplasmic reticulum (ER) or secretory pathway, and nuclear—can be used to categorize mammalian FKBPs. One PPIase domain is present in both the nuclear FKBP25 and 133 and the cytoplasmic FKBP12 and 12.6 isoforms. Multiple TPR domains are found in FKBPs 36, 38, 51, and 52. An N-terminal ER signal peptide is present in the ER FKBPs FKBP13, 19, 22, 23, 60, and 65.

FKBP related products

Structure Cat No. Product Name CAS No. Product Description
10-SLF V123024 10-SLF 2765058-89-5 10-SLF is a PROTAC FKBP12 degrading agent.
AP1867-3-(aminoethoxy) hydrochloride V109020 AP1867-3-(aminoethoxy) hydrochloride 2127390-16-1 AP1867-3-(aminoethoxy) hydrochloride is a synthetic FKBP ligand (PROTAC target protein ligand) based on AP1867.
AP1867-NH-PEG3-acid V129211 AP1867-NH-PEG3-acid AP1867-NH-PEG3-acid is a target protein ligand-linker conjugate containing the FKBP12F36V ligand AP1867 and the PROTAC linker, and can recruit E3 ligases.
AP21998 V109049 AP21998 292606-90-7 AP21998 is an Fm (mutant FKBP) domain-selective ligand that can bind to a single FKBPv.
BRD4/FKBP12 degrader-1 V130627 BRD4/FKBP12 degrader-1 BRD4/FKBP12 degrader-1 is a BRD4/FKBP12 degrader (BRD4 ligand, FKBP12 ligand, linker) with anticancer activity.
BRD4/FKBP12 degrader-2 V130628 BRD4/FKBP12 degrader-2 BRD4/FKBP12 degrader-2 is a BRD4/FKBP12 degrader with anticancer activity (BRD4 ligand, FKBP12 ligand, linker).
dTAGV-1 V120135 dTAGV-1 2451573-86-5 dTAGV-1 is a highly efficient and selective PROTAC degrader that can degrade the FKBP12F36V tagged protein.
FKBP12 ligand-2 V136062 FKBP12 ligand-2 3036243-81-6 FKBP12 ligand-2 is a high-affinity FKBP12 targeting ligand.
FKBP12 ligand-3 V136063 FKBP12 ligand-3 3036374-26-9 FKBP12 ligand-3 is a high-affinity FKBP12 targeting ligand.
FKBP12 Ligand-Linker Conjugate 1 V136064 FKBP12 Ligand-Linker Conjugate 1 2765059-01-4 FKBP12 Ligand-Linker Conjugate 1 is a conjugate composed of FKBP12 target protein ligands and linkers.
FKBP12 PROTAC FM4 V136066 FKBP12 PROTAC FM4 3115268-06-6 FKBP12 PROTAC FM4 is a PROTAC degrader of FKBP12 with a DC50 value of 0.09-0.22 nM.
FKBP51-Hsp90-IN-1 V88489 FKBP51-Hsp90-IN-1 433313-64-5 FKBP51-Hsp90-IN-1 (Compound D10) is a selective FKBP51-Hsp90 protein-protein interaction inhibitor with an IC50 of 0.1 μM for FKBP51.
FKBP51-Hsp90-IN-2 V88490 FKBP51-Hsp90-IN-2 601511-07-3 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.
MC-25B V139489 MC-25B MC-25B is a specific FKBP12 PROTAC degrader.
S107 hydrochloride V33117 S107 hydrochloride 1357476-46-0 S107 hydrochloride is a novel, potent and RyR-selective 1,4-benzothiazepine analogue that stabilizes RyR2 channels by enhancing the binding affinity of calstabin2 to mutant and/or PKA-phosphorylated channels.
SP3N V88492 SP3N SP3N is a specific degrader of proline isomerase FKBP12, which is converted into a precursor of active aldehydes (SP3CHO) by amine oxidase metabolism.
SP3N hydrochloride V145180 SP3N hydrochloride SP3N hydrochloride is a specific degrader of prolyl isomerase (FKBP12).
WAY-380153 V109065 WAY-380153 363160-12-7 WAY-380153 (compound 24) is an FKBP12 inhibitor.
长川霉素 V1936 Ascomycin (FK520) 104987-12-4 Ascomycin (also known as FK520, FR 900520, Immunomycin), a natural product isolated from Streptomyces, is anethyl analog of tacrolimus (FK506) anda neutral macrolide immunosuppressant, which prevents rejection after an organ transplant.
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