Catalog No.
Product Name
Application
Product Information
Citations
-
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.
-
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. -
Cytolysin
TAM470 is a novel cytolysin that functions by inhibiting tubulin polymerization and facilitating microtubule depolymerization. This compound serves as a valuable payload molecule in the synthesis of OMTX705, a groundbreaking antibody-drug conjugate (ADC) targeting fibroblast activation protein (FAP) and demonstrating significant antitumor activity. TAM470 is of interest for research into cancer therapeutics and the development of targeted delivery systems. -
STING Agonist
STING agonist-18 diTFA is a potent STING (Stimulator of Interferon Genes) agonist that activates the STING pathway, leading to enhanced immune responses. This compound is useful for the synthesis of antibody-drug conjugates (ADCs), enabling targeted delivery of therapeutics. Its potential applications in cancer immunotherapy and other immune-mediated therapies make it a valuable reagent for research in drug development and immunological studies. -
STING Agonist
STING agonist-49 is a powerful stimulator of the STING (Stimulator of Interferon Genes) pathway, engaging the immune response through Type I interferon production. This compound demonstrates potent biological activity in modulating immune responses, making it a valuable tool in lung cancer research. STING agonist-49 can also serve as an effective payload in antibody-drug conjugates (ADCs), enhancing targeted therapeutic approaches in various malignancies. -
STING Agonist
STING agonist-18 is a potent agonist of the stimulator of interferon genes (STING) pathway, known for its ability to activate immune responses. This compound is particularly useful in the synthesis of antibody-drug conjugates (ADCs), such as Trastuzumab conjugates, facilitating targeted therapeutic approaches. Its application in cancer immunotherapy and related research enhances the understanding of STING pathway modulation in tumor microenvironments. -
Intermediate Product
TAM558 Intermediate-5 is a pivotal intermediate in the synthesis of TAM558, which serves as the payload molecule for the formation of OMTX705. OMTX705 is a humanized antibody targeting fibroblast activation protein (FAP), facilitating cytolysis via binding to TAM470. This intermediate is essential for research into anti-tumor therapies and the development of novel cancer treatments targeting the tumor microenvironment. -
Intermediate Product
TAM558 intermediate-2 is a critical intermediate in the synthesis of TAM558, a payload molecule used in the preparation of OMTX705. OMTX705 is a humanized antibody targeting fibroblast activation protein (FAP), which exhibits significant anti-tumor activity by binding to the cytolysin TAM470. This intermediate plays a vital role in facilitating the development of innovative therapeutic agents for cancer treatment. -
COX-2/Carbonic Anhydrase Inhibitor
Polmacoxib is a novel, orally active nonsteroidal anti-inflammatory drug (NSAID) that acts as a dual inhibitor of cyclooxygenase-2 (COX-2) and carbonic anhydrase, with an IC50 value of approximately 0.1 μg/ml for COX-2. It exhibits significant biological activity by inhibiting the growth of colorectal adenomas and tumors in mouse models, making it a promising tool for cancer research. Polmacoxib is valuable for studying the roles of COX-2 and carbonic anhydrase in cancer biology and inflammation. -
COX-2 Inhibitor
COX-2-IN-30 is a benzenesulfonamide derivative that functions as a potent selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 49 nM and also inhibits 5-lipoxygenase (5-LOX) with an IC50 of 2.4 μM. Additionally, it affects human carbonic anhydrase isoforms IX and XII, displaying nanomolar Ki values. This compound demonstrates significant analgesic and anti-inflammatory properties while maintaining a favorable gastrointestinal safety profile, making it useful for research in inflammation, pain relief, and related gastrointestinal studies. -
OMTX705 Payload Molecule
TAM558 is a payload molecule utilized in the synthesis of OMTX705, a humanized anti-fibroblast-activating protein (FAP) antibody conjugated to the cytolysin TAM470. This conjugation enhances the antitumor activity of OMTX705, making it a valuable tool in cancer research. The combination of TAM558 with targeted antibodies facilitates the development of innovative therapeutic strategies against tumor-associated fibroblasts. -
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. -
Transcriptional Chemical Inducers of Proximity
JWZ-7-7-Neg1 is a transcriptional chemical inducer of proximity (TCIP) designed with negative chemical control. This compound selectively reduces the binding affinity to BRD4 and BCL6, thereby exhibiting decreased cytotoxicity in diffuse large B-cell lymphoma (DLBCL) cells compared to its counterpart, JWZ-7-7. JWZ-7-7-Neg1 serves as a valuable tool in cancer research, particularly for studies focusing on transcriptional regulation and targeted therapies. -
p300/CBP Inhibitor
KB528 is a selective inhibitor of the histone acetyltransferases p300 and CBP, demonstrating low nM IC50 values against these targets while sparing other members of the KAT family. This compound modulates the IRF4 transcriptional network, leading to decreased expression of key oncogenes such as IRF4, MYC, CAV2, and IGLL5, as well as reduced levels of IKZF3 protein. KB528 has been shown to effectively induce apoptosis in multiple myeloma cells, making it a valuable tool for research in multiple myeloma and related oncological studies. -
CD206 Targeted Fluorescent Dye
MR2-cy5 is a fluorescent dye specifically designed to target CD206, a receptor expressed on macrophages. This reagent enables precise tracking of CD206+ macrophages in various biological samples, facilitating studies in immunology and cellular biology. MR2-cy5 is ideal for applications such as flow cytometry and imaging, contributing to the understanding of macrophage function and behavior in health and disease. -
Inflammatory Pathway Inhibitor, Oxidative Stress Inhibitor, Cancer Pathway Inhibitor
Matairesinol is an orally active bioactive compound that functions as an inflammatory pathway, oxidative stress, and cancer pathway inhibitor. It effectively inhibits the phosphorylation of MAPK, JNK, and NF-κB, while downregulating RANKL-induced NFATc1 expression and activity, and suppressing the activation of the PI3K/AKT/FOXO1 pathway. Matairesinol is applicable in research on sepsis-mediated brain injury, osteoporosis, heart failure, atopic dermatitis, and various cancer models. -
Anti-Inflammatory Agent
Isodorsmanin A is an anti-inflammatory agent that effectively suppresses the production of inflammatory mediators and pro-inflammatory cytokines. This compound inhibits the phosphorylation of c-Jun N-terminal kinase (JNK) and mitogen-activated protein kinase (MAPK), contributing to its anti-inflammatory effects. Isodorsmanin A is useful in research applications focused on inflammation-related disorders and the investigation of signaling pathways involved in inflammatory responses. -
Antiinflammatory Agent
n-Butyl α-D-fructofuranoside is an anti-inflammatory agent that enhances Nrf2 activity through the activation of JNK pathways. This compound, derived from the root barks of Ulmus davidiana var. japonica, exhibits significant anti-inflammatory properties, making it a valuable tool for studying inflammation and oxidative stress in various biological systems. Its potential applications include the investigation of cellular responses to inflammation and the modulation of antioxidant pathways. -
RAS/RAS-RAF Inhibitor
RAS/RAS-RAF-IN-1 is a potent inhibitor targeting the RAS and RAS-RAF signaling pathways. With a dissociation constant (KD) in the range of 5.0 μM to 15 μM for cyclophilin A (CYPA), this compound demonstrates significant binding affinity. RAS/RAS-RAF-IN-1 exhibits notable antitumor activity, making it a valuable tool for cancer research and therapeutic development. -
Anti-Inflammatory Agent
Rhamnocitrin is an anti-inflammatory and antioxidant agent that targets the STIM-1, NFATc3, and MAPK pathways. It effectively scavenges free radicals and exhibits a specific inhibitory effect on oxidative stress and inflammatory responses in vascular endothelial cells and neurons. Through upregulation of miR-185, Rhamnocitrin inhibits STIM-1-mediated store-operated calcium entry, which prevents NFATc3 translocation to the nucleus and reduces the expression of downstream inflammatory factors. Additionally, it induces heme oxygenase HO-1 expression and modulates the ERK/p38 MAPK pathway, mitigating the production of pro-inflammatory cytokines and adhesion molecules. Rhamnocitrin is suitable for research focused on endothelial-related inflammatory diseases and neuroprotection. -
Anti-Inflammatory Agent
Andrograpanin is a bioactive compound derived from Andrographis paniculata, acting primarily as an anti-inflammatory agent. This molecule demonstrates significant anti-inflammatory and anti-infectious properties, making it a valuable tool for research in inflammatory diseases and infections. Its mechanism of action enables the modulation of inflammatory pathways, providing insight for therapeutic development in related conditions. -
Anti-inflammatory/Anti-fibrotic Agent
GDC-3280 is an orally active anti-inflammatory and anti-fibrotic agent that operates primarily through the inhibition of the ASK1-p38 MAPK pathway. It effectively mitigates the inflammatory and fibrotic responses associated with silicosis and influences macrophage polarization. GDC-3280 is a valuable tool for research aimed at understanding and developing therapeutic strategies for inflammatory and fibrotic diseases. -
Dye/P2×7R Antagonist
Brilliant Blue G-250 is a dye that functions as a P2×7 receptor (P2×7R) antagonist. It exhibits selective inhibition of P2×7R, leading to the inactivation of the NLRP3 inflammasome, which is crucial in inflammatory processes. This compound is widely utilized for protein visualization in SDS-PAGE, providing a straightforward staining method alongside high quantitation capabilities in the Bradford protein assay, where protein concentrations are assessed by measuring absorbance at 595 nm. -
Anti-inflammatory Agent
Selenomethylene blue is an antioxidant with potent anti-inflammatory properties. It has been shown to effectively inhibit inflammatory paw edema in rodent models, making it a valuable tool for studying inflammation-related pathways. Its applications extend to research in chronic inflammatory conditions and potential therapeutic interventions. -
Antiviral Agent
Brilliant Black BN is an azo dye with a notable application as an antiviral agent. It effectively inhibits the interaction between enterovirus 71 (EV71) and its uncoating factor, cyclophilin A, demonstrating significant potential in the treatment of viral infections. This compound serves as a valuable tool for research focused on antiviral mechanisms and infectious disease studies. -
WNT7A Inhibitor/Photosensitizer
WNT7A-IN-1 sodium is a selective inhibitor of WNT7A that disrupts the interaction between WNT7A and its receptor FZD5, leading to enhanced expression of MHC-I. This reagent is known to significantly increase levels of MHC-I and phosphorylated p65 while decreasing active β-catenin expression. Additionally, WNT7A-IN-1 sodium acts as a photosensitizer in the green spectral region, making it suitable for applications in photodynamic therapy and immunological studies. -
Arginase Inhibitor
nor-NOHA monoacetate is a selective and reversible inhibitor of arginase. It induces apoptosis in cells expressing arginase 2 under hypoxic conditions and demonstrates anti-leukemic activity. This compound is valuable for investigating endothelial dysfunction, immunosuppression, and metabolic processes in various biological contexts. -
Arginase Inhibitor
ABH hydrochloride is a potent arginase inhibitor with a Ki value of 8.5 nM. This compound enhances nitric oxide production and downregulates inflammatory mediators, including ICAM-1, VCAM-1, and MCP-1. ABH hydrochloride is utilized in research focused on erectile dysfunction, lung protection, wound healing, blood pressure regulation, and vascular fibrosis. Its dual role in promoting vasodilation and reducing inflammation makes it a valuable reagent for studying cardiovascular and inflammatory diseases. -
Arginase Inhibitor
OATD-02 is a competitive, reversible, noncovalent inhibitor that targets arginase 1 and 2. It exhibits slow offset kinetics with IC50 values of 20 nM for human arginase 1, 39 nM for human arginase 2, 39 nM for mouse arginase 1, and 28 nM for rat arginase 1. OATD-02 effectively disrupts tumor immunosuppression mediated by arginases, making it a valuable tool for research in melanoma and other cancer immunotherapy studies. -
Arginase Inhibitor
ARG1-IN-1 is a potent arginase inhibitor with an IC50 value of 29 nM. This compound effectively inhibits serum arginase activity, leading to increased levels of arginine in various mouse tumor models. ARG1-IN-1 is particularly useful for research applications focused on tumor biology and arginine metabolism in cancer.
