Catalog No.
Product Name
Application
Product Information
Citations
- 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 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 Dimerizer
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. -
heterobifunctional degrader
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. -
FKBP ligand
AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules. -
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. -
FKBP substrate
Suc-Ala-Leu-Pro-Phe-pNA (Suc-ALPF-pNA) is a substrate of FK-506 binding protein (FKBP). -
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. -
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. -
Stable Isotope
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. -
E3 Ligase Ligand-linker Conjugate
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. -
E3 ligase ligand-linker conjugate
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. -
Stable Isotope
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. -
FKBP51-Hsp90 Interaction Inhibitor
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 Inhibitor
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. -
Stable Isotope
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. -
mTOR Inhibitor
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. -
FKBP12 Targeting AUTAC
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. -
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.
