FKBP Inhibitor

WAY-380153 (Compound 24) is an FKBP12 inhibitor. WAY-380153 exhibits moderate binding affinity for FKBP12, with a KD of 19 μM (measured by ITC) and 15 μM (measured by NMR). WAY-380153 can be used in research related to neurotrophy and neuroprotection.

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.

Ascomycin (Immunomycin; FR-900520; FK520) is an ethyl analog of Tacrolimus (FK506) with strong immunosuppressant properties. Ascomycin is also a macrocyclic polyketide antibiotic with multiple biological activities such as anti-malarial, anti-fungal and anti-spasmodic. Ascomycin prevents graft rejection and has potential for varying skin ailments research.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a FKBP12^F36V PROTAC degrader. FKBP12 PROTAC dTAG-7 binds FKBP12^F36V and CRBN to form a complex, mediating degradation via the ubiquitin-proteasome system. FKBP12 PROTAC dTAG-7 mediates the degradation of FKBP12^F36V-tagged nuclear and cytoplasmic proteins, including BRD4, HDAC1, EZH2, MYC, PLK1, KRAS^G12V, and antigen fusion proteins. FKBP12 PROTAC dTAG-7 enhances MHC class I antigen presentation. FKBP12 PROTAC dTAG-7 is applicable to leukemia-related research.

AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12^F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules.

dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF (HY-114872) of FKBP12, the Thalidomide based Cereblon ligand and a linker.

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

KB02-SLF is a nuclear FKBP12 covalent PROTAC degrader. KB02-SLF covalently modifies cysteine residues in DCAF16, forms a ternary complex with nuclear FKBP12, and mediates degradation via the CUL4-DDB1 E3 ubiquitin ligase pathway. KB02-SLF promotes polyubiquitination and proteasomal degradation of nucleus-localized FKBP12. KB02-SLF can be used in breast cancer research.

ElteN378 is an inhibitors of FKBP12e. ElteN378 can be used in study Alzheimer disease, Parkinson disease, Amyotrophic Lateral Sclerosis, proliferation disorders and cancer.

Ascomycin (Standard) is the analytical standard of Ascomycin. This product is intended for research and analytical applications. Ascomycin (Immunomycin; FR-900520; FK520) is an ethyl analog of Tacrolimus (FK506) with strong immunosuppressant properties. Ascomycin is also a macrocyclic polyketide antibiotic with multiple biological activities such as anti-malarial, anti-fungal and anti-spasmodic. Ascomycin prevents graft rejection and has potential for varying skin ailments research[1][2].

FKBP51-Hsp90-IN-1 (Compound D10) is a selective inhibitor of the FKBP51-Hsp90 protein-protein interaction, with an IC₅₀ value of 0.1 μM against FKBP51. FKBP51-Hsp90-IN-1 can be used in the research of stress-related diseases, Alzheimer's disease, and metabolic disorders.

Setafrastat (Compound 40) is a hair growth stimulator.

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

L 683519, one of the impurities of tacrolimus, is an immunosuppressant. L 683519 can inhibit the activity of FK-506 binding protein.

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.

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.

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.

SAFit1 (Standard) is the analytical standard of SAFit1 (HY-102079). This product is intended for research and analytical applications. SAFit1 is a FK506 binding protein 51 (FKBP51)-specific inhibitor with a K_i of 4±0.3 nM.