FKBP

FKBP (FK506-binding protein) is one of two major immunophilins and most of FKBP family members bind FK506 and show peptidylprolyl cis/trans isomerase (PPIase) activity. Small size FKBP family members contain only FK506-binding domain, while FKBPs with large molecular weights possess extra domains such as tetratricopeptide repeat domains, calmodulin binding and transmembrane motifs. 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.

FK506-binding proteins 1a and 1b (FKBP1a/1b) are immunophilin proteins that bind the immunosuppressant agent FK506 and AY 22989. FKBP12 is a ubiquitous abundant protein that acts as a receptor for FK506, binds tightly to intracellular calcium release channels and to the transforming growth factor β (TGF-β) type I receptor.

Targets for FKBP

Products for FKBP

Cat.No. Product Name Information
GC34172 AP1867 AP1867 is a synthetic FKBP12F36V-directed ligand.
GC61745 AP1867-2-(carboxymethoxy)

PROTAC FKBP12-binding moiety 2
AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules.
GC15586 AP1903

AP1903
AP1903 is a bivalent "dimerizer" compound that binds FKBP and induces Fas cross-linking.
GC14498 AP20187

B/B Homodimerizer
AP20187 is a synthetic dimerizer compound that can induce the dimerization of proteins engineered to contain FKBP (FK506-binding protein) domains. AP20187 has been widely used in various biological research and therapeutic applications to control protein-protein interactions and regulate cellular processes.
GC13215 Ascomycin(FK 520)

Changchuanmycin, FK-520, FR900520, Immunomycin, L 683590
Ascomycin(FK 520) is a pharmacologically active 23-membered macrocyclic polyketide antibiotic with immunosuppressive, antimalarial, and antifungal activities.
GC13601 Everolimus (RAD001)

RAD001
Everolimus (RAD001) is an orally effective second-generation mTOR inhibitor.
GC39809 GPI-1485 GPI-1485 is a non-immunosuppressive FKBP52-specific ligand.
GC62186 KB02-SLF 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.
GC39503 PROTAC FKBP Degrader-3 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.
GC73491 RapaBlock

ZZY05-092
RapaBlock is a potent, non-immunosuppressive and brain-impermeable FKBP12 ligand.
GC15031 Rapamycin (Sirolimus)

AY 22989, NSC 226080, Sirolimus, Wy 090217
Rapamycin (Sirolimus) is a macrolide mTOR inhibitor (IC₅₀=0.1nM).
GC48027 Rapamycin-d3

Sirolimus-d3
An internal standard for the quantification of rapamycin
GC33699 SAFit1 SAFit1 is a FK506 binding protein 51 (FKBP51)-specific inhibitor with a K_i value of 4 ± 0.3nM.
GC34093 SAFit2 SAFit2 is a potent inhibitor of FK506-binding protein 51 (FKBP51), with the K_ivalue of 6nM.
GC38060 Shield-1

Shld1
Shield-1 is a specific, cell-permeable ligand for FK506-binding protein 12 (FKBP).
GC44899 SLF

Synthetic Ligand of FKBP
FK-506 is a potent immunosuppressant that forms a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12).
GC61461 SLF TFA 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.
GC16233 Tacrolimus (FK506)

Tacrolimus

Tacrolimus (FK506), a macrolide antibiotic with potent immunosuppressive effects was isolated from Streptomyces tsukubaensis and has been previously used to prevent allograft and for treatment of autoimmune disorders in humans.
GC17995 Tacrolimus monohydrate immunosuppressive drug
GC33200 Target Protein-binding moiety 13

PROTAC FKBP12-binding moiety 1
Target Protein-binding moiety 13 (PROTAC FKBP12-binding moiety 1) is a synthetic ligand for FKBP (SLF). Target Protein-binding moiety 13 (PROTAC FKBP12-binding moiety 1) can be used in the synthesis of PROTACs.
GC66370 Zapalog 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.