Catalog No.
Product Name
Application
Product Information
Citations
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mTOR Inhibitor
RapaLink-1 is a third-generation bivalent inhibitor targeting the mechanistic target of rapamycin (mTOR). By combining Rapamycin with MLN0128 through an inert linker, RapaLink-1 demonstrates superior efficacy in inhibiting both wild-type and mutant forms of mTOR compared to other inhibitors. This compound effectively crosses the blood-brain barrier, promoting durable mTORC1 inhibition via FKBP12 binding. Additionally, RapaLink-1 exhibits anticancer properties and may play an antithrombotic role in antiphospholipid syndrome by enhancing autophagy. -
mTOR Inhibitor/Autophagy Inducer
mTOR inhibitor-8 is a potent inhibitor of the mechanistic target of rapamycin (mTOR), functioning through the interaction with FKBP12. This compound effectively suppresses mTOR activity and induces autophagy in A549 human lung cancer cells. It is a valuable tool for studying mTOR signaling pathways and the role of autophagy in cancer research. -
FKBP12 Inhibitor
WAY-380153 is an FKBP12 inhibitor that demonstrates moderate binding affinity for FKBP12, with a KD of 19 μM measured via isothermal titration calorimetry and 15 μM via nuclear magnetic resonance. This compound is relevant for research applications involving neurotrophy and neuroprotection, serving as a valuable tool for investigating conditions related to neuronal health and function. -
FKBP51 Degrader, VHL Binder
SelDeg51 is a selective PROTAC degrader targeting FKBP51 with a Kd value of 18 nM and a maximum degradation efficacy (Dmax) of 90%. It facilitates the proteasomal degradation of FKBP51 through the formation of a ternary complex with FKBP51 and VHL, effectively reactivating glucocorticoid receptor signaling. SelDeg51 is particularly relevant for research in stress-related mental disorders, chronic pain, and obesity. -
Ligand for Target Protein for PROTAC
AP1867-3-(aminoethoxy) hydrochloride is a synthetic ligand targeting FKBP and plays a crucial role in the development of PROTAC-based therapies. This compound is utilized in the synthesis of PROTAC FKBP12 F36V degraders, facilitating targeted protein degradation. Its application extends to research in therapeutic modalities that employ ubiquitin-proteasome system for regulating protein levels in various diseases. -
FKBP Ligand
SLF is a synthetic ligand specifically targeting FK506-binding protein (FKBP), exhibiting an affinity of 3.1 μM for FKBP51 and an IC50 of 2.6 μM for FKBP12. This compound serves as a valuable tool in the development of PROTACs, enabling selective degradation of target proteins. Its application in chemical biology research facilitates the exploration of protein regulation and therapeutic strategies. -
FKBP12 Ligand
RapaBlock is a potent FKBP12 ligand that does not exert immunosuppressive effects and is characterized by its inability to penetrate the blood-brain barrier. This compound is primarily utilized in research to investigate FKBP12-related pathways and functions, offering valuable insights into cellular signaling mechanisms while minimizing unintended effects in neural tissue. -
FKBP12F36V PROTAC Degrader
dTAGV-1 is a selective proteolysis-targeting chimera (PROTAC) degrader designed to target FKBP12F36V-tagged proteins. This compound effectively induces the degradation of FKBP12F36V-Nluc in vivo, making it a valuable tool for studying protein turnover and function. Its application is particularly relevant in cellular and molecular biology research, facilitating the investigation of protein interactions and therapeutic targets. -
Ligand for Target Protein for PROTAC
AP1867-3-(aminoethoxy) is a synthetic ligand that targets FKBP, facilitating the design of PROTAC molecules. This compound is essential for the synthesis of the PROTAC FKBP12 F36V degrader, enabling targeted protein degradation in various biological contexts. Its use is crucial in research applications focused on protein regulation and therapeutic development. -
FKBP12 Inhibitor
ElteN378 is a selective inhibitor of FKBP12. This compound has demonstrated significant biological activity in the modulation of protein folding and signaling pathways. Research applications include investigations into neurodegenerative diseases such as Alzheimer's and Parkinson's, as well as studies on amyotrophic lateral sclerosis, proliferation disorders, and various cancer types. -
FKBP Ligand
SLF TFA is a synthetic ligand specifically targeting FK506-binding proteins (FKBPs), exhibiting an affinity of 3.1 μM for FKBP51 and an IC50 value of 2.6 μM for FKBP12. This compound is pivotal in research applications involving the development of PROTACs (proteolysis-targeting chimeras), which facilitate targeted protein degradation. Its selective interaction with FKBPs underscores its potential utility in studying protein regulation and cellular processes. -
Target Protein Ligand-Linker Conjugate
FKBP12 Ligand-Linker Conjugate 1 is designed to bind the FKBP12 protein, serving as a critical component in targeted protein degradation applications. This conjugate facilitates the synthesis of PROTAC degrader MC-25B, enabling researchers to study the modulation of protein levels within cellular systems. Its utility in chemical biology makes it a valuable tool for investigating protein interaction dynamics and therapeutic development. -
Immunosuppressive Modulator
ILS-920 is an immunosuppressive modulator and a nonimmunosuppressive analog of Rapamycin, designed to exhibit reduced immunosuppressive effects while retaining neuroprotective properties. It selectively binds to FKBP52 and the β1-subunit of L-type voltage-gated calcium channels (VGCC), demonstrating a remarkable 200-fold selectivity for FKBP52 over FKBP12. This compound is of particular interest in research areas focusing on neuroprotection and the modulation of calcium signaling pathways. -
FKBP12 Ligand
FKBP12 ligand-2 is a high-affinity ligand that selectively targets FKBP12. This compound enhances the binding of heterobifunctional molecules to BRD4, facilitating the formation of a ternary complex of FKBP12, ligand, and BRD4 through the "CellTrap" effect. The resulting complex exhibits inhibitory activity against BRD4, leading to the downregulation of BRD4 target genes such as MYC and promoting cancer cell apoptosis. FKBP12 ligand-2 is suitable for research applications focused on cancer mechanisms influenced by intracellular protein levels. -
FKBP51 F67V Antagonist Ligand
FKBP51F67V-selective antagonist Ligand2 is a potent ligand specifically targeting the FKBP51 F67V variant. It effectively reverses the anxiogenic phenotype induced by the overexpression of FKBP51 F67V in the amygdala, thereby highlighting its potential in anxiety research. This compound selectively binds to FKBP51 F67V without interacting with wild-type FKBP51 or FKBP52, making it a valuable tool for studying the specific roles of FKBP51 F67V in neurobiology and related disorders. -
PROTAC FKBP12 Degrader
10-SLF is a PROTAC FKBP12 degrader that facilitates the formation of a ternary complex between FKBP12 and the mutant E3 ligase FBXW7-R465C. This compound promotes the FBXW7-R465C-mediated proteasomal degradation of FKBP12, selectively lowering FKBP12 levels in cells harboring the FBXW7-R465C mutation. 10-SLF is valuable for studying protein degradation pathways and the role of FKBP12 in various biological contexts. -
FKBP12 Ligand
FKBP12 ligand-3 is a high-affinity ligand that selectively targets FKBP12. By facilitating the binding of heterobifunctional molecules to BRD4, it enhances intracellular drug enrichment through the "CellTrap" effect, leading to the formation of a ternary complex of FKBP12-ligand-BRD4. This complex exhibits inhibitory effects on BRD4, resulting in the downregulation of target genes such as MYC and promoting tumor cell apoptosis. FKBP12 ligand-3 is valuable for research focused on cancer therapeutics, particularly in studies that exploit variations in intracellular presenter protein levels. -
FKBP12 Ligand
FKBP12 Ligand-1 is a specific ligand designed to target FKBP12, facilitating the selective recruitment of proteins for ubiquitin-mediated degradation. This compound is primarily utilized in research applications involving proteolysis-targeting chimera (PROTAC) technology, particularly with MC-25B. FKBP12 Ligand-1 serves as a vital tool for studying protein degradation pathways and examining the functional dynamics of cellular targets.
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Nucleoprotein PROTAC Degrader
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. -
Fv Domain-Selective Lligand
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. -
FKBP12 PROTAC Degrader
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. -
Immunosuppressant
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. -
FKBP12 Ligand
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. -
FKBP35 Inhibitor
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. -
FKBP52 Targeting Agents
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. -
FKBP (F36V) Ligand
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. -
BRD4/FKBP Binding Agent
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. -
AUTAC Ligand
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. -
PROTAC Degrader for FKBP12
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. - Pimecrolimus is a natural ascomycin macrolactam that binds to macrophilin-12 (FKBP-12) and inhibits calcineurin as well as prolyl isomerase (rotamase).
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FKBP substrate
Suc-Ala-Leu-Pro-Phe-pNA (Suc-ALPF-pNA) is a substrate of FK-506 binding protein (FKBP). -
PROTAC FKBP12 Degrader
FKBP12 PROTAC RC32 is a targeted protein degrader utilizing PROTAC technology to selectively degrade FKBP12. This compound combines Rapamycin, a well-characterized immunosuppressant, with a Cereblon E3 ubiquitin ligase ligand derived from Pomalidomide, facilitating the ubiquitination and subsequent proteasomal degradation of FKBP12. It serves as an important tool in research applications aimed at investigating the modulation of protein levels and the functional consequences of targeted degradation in various biological contexts. -
FKBP12F36V PROTAC Degrader
dTAGV-1 hydrochloride is a highly selective degrader targeting FKBP12F36V-tagged proteins through the PROTAC mechanism. This compound effectively induces the degradation of FKBP12F36V-Nluc in vivo, making it a valuable tool for studies involving targeted protein degradation. Its application in research facilitates the investigation of protein function, dynamics, and the development of therapies that exploit the proteolysis pathway. -
PROTAC FKBP12 Degrader
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader designed to facilitate targeted protein degradation. It achieves this by covalently modifying DCAF16, an E3 ligase, thereby enhancing the stability of FKBP12 degradation within biological systems. The compound consists of a molecular glue linking the ubiquitin E3 ligase ligand KB02 with SLF, enabling efficient degradation of FKBP12 for various research applications in protein regulation and degradation pathways. -
FKBP12(F36V) Inhibitor
dTAGV-1-NEG is a diastereomer that acts as a heterobifunctional negative control for dTAGV-1, specifically targeted at FKBP12(F36V). This compound is utilized in research to study the selectivity and efficacy of FKBP12(F36V) degraders, helping to elucidate cellular mechanisms and pathways influenced by FKBP12 modulation. Its role as a control reagent makes it essential for validating experimental results in protein degradation studies. -
dTAG-13 Negative Control
dTAG-13-NEG serves as a negative control for dTAG-13, a PROTAC-based bifunctional degrader that selectively targets FKBP12F36V in the presence of a protein of interest. While dTAG-13 promotes the degradation of FKBP12F36V, dTAG-13-NEG allows for the assessment of specificity and background in experimental setups involving this pathway. This compound is essential for validating experimental results when studying protein degradation mechanisms and their implications in cellular biology. -
PROTAC FKBP Degrader
PROTAC FKBP Degrader-3 is a proteolysis-targeting chimera that utilizes a FKBP ligand binding group and a von Hippel-Lindau (VHL) E3 ligase recruiting moiety linked by a flexible linker. This compound effectively induces the degradation of FKBP12, demonstrating potent biological activity in targeted protein degradation. It is primarily used in research applications related to protein homeostasis, cellular signaling mechanisms, and therapeutic development strategies for modulating protein levels. -
FKBP12F36V Degrader
dTAG-47 is a heterobifunctional degrader that selectively targets FKBP12^F36V-tagged proteins for degradation. By binding FKBP12^F36V, which acts as a degradation tag (dTAG), dTAG-47 enables conditional and selective protein degradation. It is a valuable tool for studying protein function in models such as basal-like breast cancer (BBC). -
FKBP12F36V degrader
dTAGV-1 TFA is a potent and selective degrader of FKBP12^F36V-tagged fusion proteins. It enables efficient in vivo degradation of FKBP12^F36V-Nluc, making it a valuable tool for conditional protein degradation studies in live models. -
FKBP12F36V degrader
dTAG-13 is a PROTAC-based heterobifunctional degrader that selectively targets FKBP12^F36V fused in-frame to a protein of interest. By engaging both FKBP12^F36V and the cereblon (CRBN) E3 ligase, dTAG-13 induces efficient and selective degradation of FKBP12^F36V-tagged proteins, making it a valuable tool for conditional protein knockdown studies. -
FKBPL Peptide
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. -
EWSR1::FLI1 Binder
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. -
FKBP dimerizer
AP1903 is a lipid-permeable tacrolimus analogue with homodimerizing activity. Dimerizer drug AP1903 homodimerizes an analogue of human protein FKBP12 (Fv) which contains a single acid substitution (Phe36Val) so that AP1903 binds to wild-type FKBP12 with 1000-fold lower affinity. -
FKBP ligand
SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) is a synthetic ligand for FKBP (SLF). SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) can be used in the synthesis of PROTACs.
