FKBP

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.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader.

AP1867 is a synthetic FKBP12F36V-directed ligand.

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

Thalidomide-4-O-C6-NH2 hydrochloride is an E3 ligase ligand-linker conjugate that plays a critical role in the targeted protein degradation (PROTAC) system, specifically in dTAG-13 applications. This compound is utilized for its ability to degrade FKBP12F36V and bromodomain and extraterminal (BET) proteins, facilitating the modulation of various cellular processes. Its utility in research allows for advancements in understanding protein function and the development of therapeutic strategies.

Everolimus-d4 is a deuterium-labeled derivative of Everolimus, a potent and selective inhibitor of mTOR1. By binding to FKBP-12, Everolimus-d4 forms an immunosuppressive complex that effectively inhibits tumor cell proliferation, while simultaneously inducing apoptosis and autophagy. This stable isotope is valuable for research applications in oncology and immunology, facilitating studies on the therapeutic mechanisms and metabolic pathways associated with mTOR inhibition.

Thalidomide-4-O-C6-NH2 TFA is a synthetic E3 ligase ligand-linker conjugate designed for use in targeted protein degradation applications. This compound plays a critical role in the PROTAC dTAG-13, facilitating the selective degradation of FKBP12F36V and BET proteins. Its unique structural features allow for efficient recruitment of E3 ligases, making it a valuable tool in cellular studies of protein regulation and degradation pathways.

FKBP51-Hsp90-IN-1 is a selective inhibitor targeting the FKBP51-Hsp90 protein-protein interaction, exhibiting an IC50 value of 0.1 μM against FKBP51. This compound is valuable for research into stress-related diseases, Alzheimer's disease, and various metabolic disorders, owing to its ability to modulate protein interactions critical for cellular stress responses and stability. Its specificity makes it a potent tool for elucidating the role of FKBP51 in disease mechanisms.

FKBP51-Hsp90-IN-2 is a selective inhibitor of the FKBP51-Hsp90 protein-protein interaction, demonstrating IC50 values of 0.4 µM for FKBP51 and 5 µM for FKBP52. This compound has been shown to enhance cellular energy metabolism and promote neurite growth. Its efficacy makes FKBP51-Hsp90-IN-2 a valuable tool in research focused on neurodegenerative diseases and cancer.

Tacrolimus-13C,d2 is a stable isotope-labeled form of Tacrolimus, a macrocyclic lactone that targets FK506 binding protein (FKBP). This compound forms a complex that inhibits calcineurin phosphatase activity, thereby blocking T-lymphocyte signal transduction and interleukin-2 (IL-2) transcription. Its potent immunosuppressive properties make it valuable for research in immunology and transplantation studies.

Rapamycin-d3 is a deuterium-labeled analog of Rapamycin, a highly potent and selective inhibitor of the mechanistic target of rapamycin (mTOR), exhibiting an IC50 of 0.1 nM in HEK293 cells. It functions by binding to FKBP12, leading to allosteric inhibition of mTORC1. This compound is notable for its roles in autophagy activation and immunosuppression, making it valuable for various research applications including cancer biology, metabolic disorders, and studies of cellular growth and proliferation.

AUTAC2 is an FKBP12-targeting autophagy-mediated degrader designed to promote selective degradation of specific proteins. This compound incorporates a p-Fluorobenzyl Guanine (FBnG) moiety and an SLF ligand, which non-covalently binds to FKBP12. AUTAC2 facilitates the targeted removal of proteins through the autophagy pathway, making it a valuable tool for research applications focused on protein homeostasis and cellular regulation.

Everolimus-13C2,d4 is a stable isotope-labeled derivative of Everolimus, a potent and selective inhibitor of mTOR1. By binding to FKBP-12, Everolimus forms an immunosuppressive complex that effectively inhibits tumor cell proliferation while promoting apoptosis and autophagy. This compound is valuable for research applications in cancer therapy and immunosuppression studies, facilitating tracking and quantification in metabolic and pharmacokinetic investigations.

RA190-PEG1-NH2 is an E3 ligase ligand and a derivative of RA190. This compound is utilized in the synthesis of FKBP12 PROTAC degrader RAFKBP12, facilitating targeted protein degradation through the modulation of E3 ligase activity. Its application supports research into the development of proteolysis-targeting chimeras (PROTACs) and advances studies in cellular protein regulation.

MY-11B is a ligand for DCAF1, specifically exhibiting reactivity with the DCAF1_C1113 domain. This compound effectively inhibits YT41R and YT47R-mediated degradation of HA-FKBP12, making it a valuable tool in studying protein degradation pathways. MY-11B is also applicable in the synthesis of PROTACs, contributing to the development of targeted protein degradation strategies in chemical research.

L-Pyrohomoglutamic acid is an amino acid building block that serves as a precursor in the synthesis of ligands for FK506-binding proteins (FKBPs) and histone deacetylase (HDAC) inhibitors. This compound demonstrates key biological activity relevant to the modulation of protein functions and epigenetic regulation. Its versatile applications make it a valuable tool in chemical biology and medicinal chemistry research.

FKBP12 PROTAC FM4 is a potent PROTAC degrader targeting FKBP12 with demonstrated efficacy in inducing degradation of the MTH1 protein. Its DC50 value ranges from 0.09 to 0.22 nM, effectively inhibiting global protein synthesis and promoting apoptosis in cervical cancer cells that express MTH1-E6 and FKBP12F36V-tagged SARS1. This compound is particularly relevant for research focused on HPV-positive cervical cancer, providing valuable insights into therapeutic strategies against this malignancy.

Tacrolimus impurity 4 is a chemical impurity derived from the immunosuppressive drug Tacrolimus, primarily targeting FKBP12, a key protein involved in T-cell activation. This impurity serves as an important reference standard in quality control and analytical studies focused on the purification and characterization of Tacrolimus formulations. Its analysis aids in ensuring the safety and efficacy of Tacrolimus preparations in pharmaceutical research and development.

EcDHFR/FKBP12 F36V binder-1 is a bifunctional molecule designed to target the Escherichia coli dihydrofolate reductase (EcDHFR) domain and the FKBP12 F36V domain. This compound exhibits significant biological activity by acting as an efficient linker between the two protein domains, facilitating studies of protein-protein interactions and enabling the development of synthetic biological systems. Its applications include protein engineering, understanding signaling pathways, and advancing drug discovery efforts.