FKBP

KB03-SLF is an electrophilic PROTAC degrader targeting DCAF16 to facilitate the degradation of the nuclear protein FKBP12. This compound serves as a valuable tool in cancer research, enabling the investigation of protein homeostasis and degradation pathways. KB03-SLF’s unique structure incorporates specific ligands that enhance its efficacy as a degradative agent, making it a significant asset for studies focused on targeted protein elimination.

AP21998 is a selective ligand for the Fv domain of mutant FKBP, primarily targeting FKBPv. This compound effectively disrupts FKBP-mediated oligomerization, leading to the inhibition of proliferation in transformed myeloid progenitors while promoting their terminal myeloid differentiation. Additionally, AP21998 facilitates the resolution of aggregates in CAD-hM1 receptor fusion proteins, enabling their transit from the endoplasmic reticulum to the plasma membrane. Its unique properties make it valuable for research in cancer biology and related fields.

RAFKBP12 is a PROTAC degrader that specifically targets FKBP12, utilizing the CAP-TAC strategy to facilitate proteasome-dependent degradation. This compound operates independently of E3 ubiquitin ligases and protein ubiquitination, demonstrating its innovative mechanism of action. RAFKBP12 serves as a valuable tool for research in protein degradation pathways and therapeutic applications related to FKBP12 modulation.

L 683519 is an immunosuppressant that primarily targets FK-506 binding protein (FKBP). It functions by inhibiting the activity of FKBP, which plays a crucial role in regulating immune responses. This compound is useful for studying immunosuppressive mechanisms and can provide insights into therapies related to organ transplantation and autoimmune diseases.

MP-010 is a potent FKBP12 ligand that modulates cytosolic calcium levels by stabilizing ryanodine receptor (RyR) channel activity. This compound has been shown to enhance functional outcomes in SOD1G93A amyotrophic lateral sclerosis (ALS) mouse models, evidenced by improved motor coordination, enhanced integrity of neuromuscular junctions, and increased survival of spinal motor neurons. MP-010 serves as a valuable tool in the investigation of neurological disorders and the underlying mechanisms of ALS.

D44 is a selective inhibitor of FKBP35, targeting the PPIase activity essential for Plasmodium survival. With IC50 values of 132 nM for Plasmodium falciparum and 125 nM for Plasmodium vivax, D44 demonstrates significant antiplasmodium activity. This compound is valuable for research applications focused on malaria and other infectious diseases, providing insights into potential therapeutic approaches.

MJC13 is an FKBP52-targeted agent that exhibits anti-tumor activity, making it a valuable tool in prostate cancer research. By selectively interacting with FKBP52, MJC13 may influence cancer cell proliferation and survival. This reagent is suitable for studies investigating the role of FKBP52 in cancer biology and therapeutic approaches targeting this mechanism.

Shield-2 is a potent stabilizing ligand that specifically targets the FKBP (F36V) protein, exhibiting a dissociation constant of 29 nM. This compound effectively binds to FKBP mutants, which destabilize protein domains and subsequently prevents their degradation. Shield-2 offers a valuable tool for researchers studying intracellular protein regulation and the modulation of protein levels within cellular environments.

HLDA-221 is a non-covalent regulated induced proximity targeting agent (RIPTAC) that selectively binds to BRD4-BD1 upon pre-incubation with FKBP. This compound facilitates protein-protein interactions, making it a valuable tool for studying cellular signaling pathways and gene regulation. HLDA-221 has potential applications in cancer research, particularly in understanding the role of BRD4 in tumorigenesis and therapeutic targeting.

TSPO ligand-3 serves as a ligand for AUTAC2, which features a p-fluorobenzylguanine (FBnG) moiety alongside a synthetic FKBP ligand (SLF). This compound exhibits notable biological activity by significantly silencing FKBP12 in HeLa cells. Research applications include studying targeted protein degradation and investigating the mechanistic pathways of autophagy-related and intracellular degradation processes.

22-SLF is a PROTAC degrader specifically targeting FK506-binding protein 12 (FKBP12), exhibiting a DC50 of 0.5 µM. This compound forms a ternary complex with C227 and C228 in FBXO22, facilitating FKBP12 degradation in an FBXO22-dependent manner. 22-SLF is a valuable tool for cancer research, serving as a probe to investigate the FBXO22-mediated degradation pathways.

AD 01 is a 24-amino acid peptide derived from FKBPL (FK506-binding protein like), targeting the CD44 receptor to exert significant anti-angiogenic effects. By binding to CD44, AD 01 effectively inhibits tumor cell migration in a manner dependent on this receptor. This peptide is valuable for research applications focused on cancer biology, particularly in studies related to angiogenesis and tumor metastasis.

EB-TCIP is an EWSR1::FLI1 binder that operates by forming a ternary complex with the tagged fusion protein BCL6 and FKBP12F36V. This compound specifically recruits the EWSR1::FLI1 fusion to BCL6-associated DNA regions, leading to chromatin remodeling and the relocalization of transcriptional factors. As a result, EB-TCIP activates the expression of previously repressed BCL6 target genes. It serves as a valuable tool in the exploration of innovative epigenetic therapies for Ewing sarcoma.

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.

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.

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.

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.

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.