Catalog No.
Product Name
Application
Product Information
Citations
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5-LOX/COX Inhibitor
(-)-Bornyl ferulate serves as a dual inhibitor of 5-lipoxygenase (5-LOX) and cyclooxygenase (COX), displaying IC50 values of 10.4 μM and 12.0 μM, respectively. This compound demonstrates significant anti-inflammatory potential, making it useful for research focused on inflammation-related pathways and conditions. Its ability to modulate leukotriene and prostaglandin synthesis positions it as a valuable tool in the study of various inflammatory diseases and therapeutic interventions. -
COX-2 Inhibitor
Cavidine is a selective COX-2 inhibitor that exhibits potent anti-inflammatory properties. It is particularly useful in research concerning skin injuries, hepatitis, cholecystitis, and scabies. Additionally, Cavidine has been shown to alleviate LPS-induced acute lung injury through modulation of the NF-κB signaling pathway, making it a valuable compound for studying inflammation-related conditions. -
COX-2 Inhibitor
Nimesulide-d5 is a deuterated form of Nimesulide, a selective cyclooxygenase-2 (COX-2) inhibitor. It demonstrates a time-dependent inhibitory effect on COX-2 with IC50 values ranging from 70 nM to 70 μM, while exhibiting negligible activity on COX-1 (IC50 >100 μM). Nimesulide-d5 is utilized in research applications focusing on inflammatory processes, pain management, and antipyretic effects, supporting studies aimed at understanding COX-2 mediated pathways. -
COX Inhibitor
Piroxicam olamine is a non-steroidal anti-inflammatory drug that acts as an inhibitor of cyclooxygenase (COX), targeting both COX-1 and COX-2 isoforms with IC50 values of 47 μM and 25 μM, respectively, in human monocytes. This compound is primarily used in research applications focused on inflammation and analgesia. Its mechanism of action makes it a valuable tool for studying pathways involved in pain and inflammatory responses. -
Non-steroidal Anti-inflammatory Agent
Ketoprofen sodium is a non-steroidal anti-inflammatory agent that primarily targets cyclooxygenase (COX) enzymes, demonstrating inhibitory activity with IC50 values of 2 nM for COX-1 and 26 nM for COX-2. This compound is valuable in the study of inflammatory processes, immunological responses, and metabolic disorders, including obesity. Its potent anti-inflammatory properties make it a relevant tool in research aimed at understanding and mitigating these conditions. -
COX Inhibitor
COX-2-IN-1 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 3.9 μM. This compound is valuable for studying COX-2-related pathways and has applications in inflammation and pain research. By selectively targeting COX-2, it allows for the investigation of its role in various physiological and pathological processes. -
COX Inhibitor
Tilmacoxib is a highly selective, irreversible inhibitor of human COX-2, demonstrating time-dependent inhibition with an IC50 of 85 nM in enzyme assays. This compound is primarily utilized in studies investigating the role of COX-2 in inflammatory processes and related disease models. Its specificity and potency make it a valuable tool for elucidating the therapeutic potential of COX-2 inhibition in various biological contexts. -
COX Inhibitor
COX/5-LO-IN-1 is a potent inhibitor targeting cyclooxygenase (COX) and 5-lipoxygenase (5-LO), integral enzymes in the arachidonic acid pathway. This compound demonstrates significant anti-inflammatory and anti-allergic properties, making it a valuable tool for investigating the molecular mechanisms underlying inflammatory and allergic diseases. Its dual inhibition profile supports research into therapeutic strategies for various pathological conditions linked to dysregulated eicosanoid signaling. -
COX Inhibitor
SC58451 is a selective inhibitor of cyclooxygenase-2 (COX-2), known for its potency in downregulating inflammatory pathways. By specifically targeting COX-2, this compound is effective in reducing prostaglandin synthesis, making it valuable for studies related to inflammation and pain management. SC58451 is suitable for research applications in understanding diseases where COX-2 plays a critical role, such as cancer and inflammatory disorders. -
CTLA-4/PD-L1 Inhibitor
Davoceticept is a fusion protein consisting of the CD80 (1-107) fragment linked to IGHG1 Fc via a peptidyl linker, targeting CTLA-4 and PD-L1. This variant CD80 vIgD-Fc acts as an immune checkpoint inhibitor, enhancing T cell activation and promoting anti-tumor responses. Its applications include cancer immunotherapy and studying immune modulation in various malignancies, making it a valuable tool for researchers investigating therapeutic strategies in cancer treatment. -
Anti-CTLA4 Antibody
KD6001 is a humanized IgG1κ monoclonal antibody that targets CTLA-4, effectively disrupting the interactions between CTLA-4 and its ligands CD80 and CD86, with an IC50 of 16 ng/mL. This antibody promotes the activation of T cells by enhancing the expression of IL-2 and IFNγ in PHA-activated human lymphocytes. KD6001 demonstrates significant antitumor activity, inhibiting tumor growth in various mouse models, including MC38, B16, and Hepa1-6. It is relevant for research applications in cancer, particularly in advanced melanoma, hepatocellular carcinoma, and liver cancer. -
Calcineurin Inhibitor
Cyclosporin A-Derivative 1 (Free base) acts as a potent calcineurin inhibitor through its interaction with cyclophilin. This compound is derived from cyclosporin A and plays a critical role in immunosuppression by inhibiting T-lymphocyte activation. It is primarily utilized in research applications focused on transplant immunology and autoimmune disease modeling. -
Cyclosporin A Derivative
Cyclosporin A-Derivative 2 is a novel derivative of cyclosporin A known for its immunosuppressive properties. It exerts its effects by binding to cyclophilin, thereby inhibiting the activity of calcineurin. This compound is primarily utilized in research related to transplantation, autoimmune disorders, and T-cell activation. Its unique properties may facilitate studies aimed at understanding immune modulation and therapeutic interventions in related diseases. -
CypD Inhibitor
CypD-IN-4 is a potent and selective inhibitor of cyclophilin D (CypD), exhibiting high affinity with an IC50 of 0.057 μM. This compound is valuable in researching various conditions related to oxidative stress, neurodegenerative diseases, liver dysfunction, aging processes, autophagy, and diabetes. CypD-IN-4 facilitates the exploration of CypD's role in these pathologies, providing insights into potential therapeutic strategies. -
CypD Inhibitor
CypD-IN-3 is a potent and selective inhibitor of cyclophilin D (CypD), demonstrating high affinity with an IC50 value of 0.01 μM. This compound is valuable for studying a range of biological processes and diseases, including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy, and diabetes. Its specificity towards CypD makes it an important tool for elucidating the role of this target in various cellular functions and pathological conditions. -
CypE Inhibitor
CypE-IN-1 is a highly potent and selective inhibitor of cyclophilin E (CypE), exhibiting an IC50 of 0.013 μM and a Ki value of 0.072 μM. This compound is valuable for investigating the role of CypE in various pathological conditions, including oxidative stress, neurodegenerative diseases, liver disorders, aging processes, autophagy, and diabetes. Researchers can utilize CypE-IN-1 to explore therapeutic strategies targeting CypE-related pathways. -
Cyclophilin Inhibitor
CypD-IN-29 is a selective inhibitor of Cyclophilin D (CypD), with a key dissociation constant (KD) of 88.2 nM. By targeting CypD, this compound interferes with its interaction with β-amyloid protein in mitochondrial environments, thereby mitigating the formation of mitochondrial permeability transition pores (mPTP). CypD-IN-29 is suited for research focused on Alzheimer's disease mechanisms and mitochondrial dysfunction in neuronal cells. -
Cyclophilin J Inhibitor
ZX-J-19j is a selective inhibitor of cyclophilin J, a crucial target involved in various cellular processes. This compound exhibits potent antitumor activity, making it a valuable tool for cancer research. Its ability to modulate cyclophilin J function provides insights into tumor biology and potential therapeutic pathways. -
Cyclosporin A Crystalline Intermediate
Cyclosporin A-Derivative 1 is a crystalline intermediate of cyclosporin A that functions primarily by inhibiting calcineurin through binding to cyclophilin. This compound exhibits significant immunosuppressive activity, making it valuable in research related to transplantation, autoimmune diseases, and T-cell signaling. Its utility in studying the mechanisms of immune modulation further enhances its relevance in pharmacological investigations. -
FAP-binding peptide
Rofapitide tetraxetan is a highly selective fibroblast activation protein (FAP)-binding peptide, exhibiting a mean IC50 of 2.7 nM for FAP binding. This compound demonstrates significant antitumor activity and can be effectively labeled with radionuclides for use in diagnostic imaging. Its specific targeting of FAP makes it a valuable tool for research applications in cancer diagnosis and therapy. -
FAP Tracer
FAPI-46 is a quinoline-based tracer that selectively targets fibroblast activation protein (FAP). Labeled with radioactive isotopes like 68Ga or 177Lu, FAPI-46 is utilized for tumor imaging across various cancer types. Its high tumor uptake and prolonged tumor accumulation make it a valuable tool for assessing tumor burden and progression in clinical and research settings. -
FAP Inhibitor
UAMC-1110 is a highly potent and selective inhibitor of fibroblast activation protein (FAP), exhibiting an IC50 of 3.2 nM. In addition to FAP inhibition, UAMC-1110 also affects prolyl oligopeptidase (PREP) with an IC50 of 1.8 μM. This compound is primarily utilized in research applications targeting tumor microenvironment modulation and fibroblast-related pathologies. -
FAP Substrate
Suc-Gly-Pro-AMC is a fluorescent substrate designed specifically for the fibroblast activation protein (FAP). It is capable of reacting with recombinant porcine prolyl oligopeptidase, facilitating the study of FAP and prolyl endopeptidase (PREP) activity. This reagent is particularly valuable in glioma research, providing insights into the enzymatic functions associated with tumor progression and microenvironmental interactions. -
PET Tracer
FAPI-74 is a positron emission tomography (PET) tracer that specifically targets fibroblast activation protein (FAP). This compound is valuable in the study of FAP-positive tumors, enabling researchers to visualize and assess tumor metabolism and progression. FAPI-74 offers significant potential for applications in cancer imaging and therapeutic monitoring. -
FAP Radiotracer
NH2-UAMC1110 TFA is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110, designed for use as a precursor compound in the synthesis of FAP inhibitor probes. This compound incorporates an active amino group, enabling the formation of covalent bonds with various molecules, such as DOTA and radionuclide chelators, to create targeted molecular imaging probes. NH2-UAMC1110 TFA selectively binds to the FAP active site, inhibiting its serine protease activity and thereby blocking FAP-mediated tissue remodeling processes. It is particularly relevant for diagnostic imaging studies of tumors expressing FAP, including colorectal and pancreatic cancers, as well as research into FAP-related diseases like fibrosis and arthritis. -
FAP Ligand
OncoFAP is a high-affinity ligand for fibroblast activation protein (FAP), designed for targeted applications in cancer research. Its pan-tumoral potential allows for effective identification and localization of tumors, aiding in the investigation of tumor microenvironments. This reagent is particularly useful in studies focused on cancer diagnostics and therapeutics, providing a valuable tool for enhancing the precision of tumor targeting. -
FAP-targeting Ligand
Unlabeled FXX489 is a fibroblast activation protein (FAP)-targeting ligand. This compound possesses anticancer properties and can be utilized in conjunction with isotopes such as 68Ga and 177Lu for imaging and therapeutic applications. Unlabeled FXX489 is particularly relevant for research on pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), breast cancer (BC), and colorectal cancer (CRC), aiding in the exploration of FAP's role in tumor biology and treatment strategies. -
FAP Inhibitor
AZD2389 is a potent and orally active inhibitor of fibroblast activation protein (FAP). It has demonstrated significant efficacy in research related to metabolic dysfunction-associated steatohepatitis. This compound serves as a valuable tool for studying the role of FAP in metabolic diseases and may aid in the development of therapeutic strategies aimed at targeting metabolic liver disorders. -
FAP Inhibitor
FAP-IN-2 is a selective inhibitor of fibroblast activation protein (FAP), characterized by its isonitrile structure. This compound exhibits significant potential for therapeutic applications aimed at cancer treatment as well as for imaging purposes. When labeled with technetium-99m (99mTc), FAP-IN-2 can be utilized for targeted tumor single-photon emission computed tomography (SPECT) imaging, enhancing the visualization of FAP-expressing tumors. -
FAP Inhibitor
ARI-3099 is a selective fibroblast activation protein (FAP) inhibitor that targets the proteolytic activity of FAP, preventing the cleavage of human FGF-21 between residues P171 and S172. By inhibiting this activity, ARI-3099 extends the half-life of circulating human FGF-21 in murine models. This compound is relevant for research focused on type 2 diabetes and various metabolic disorders, making it a valuable tool for investigating therapeutic strategies in these areas. -
FAP ligand
FT-FAPI-12_9 is a fibroblast activation protein (FAP) ligand designed for the synthesis of FAPI-46, a radiotracer that selectively targets FAP. This compound exhibits specific binding properties that facilitate the imaging of tumors and inflammatory conditions associated with FAP expression. Its application in cancer research and molecular imaging underscores its utility in evaluating FAP as a potential therapeutic target. -
FAP Substrate
ARI-3144 is a specific substrate for fibroblast activation protein (FAP), designed for effective detection and quantification. When coupled with the fluorophore 7-Amino-4-methylcoumarin (AMC), this substrate facilitates sensitive analysis of FAP activity in various biological samples. ARI-3144 is valuable in research applications related to cancer biology and tissue remodeling, enabling deeper insights into FAP functions and its role in disease progression. -
FAP Binder
FAPI-34 is a radiolabeled imaging agent that specifically targets fibroblast activation protein (FAP). It demonstrates high affinity for FAP-expressing cells, resulting in significant internalization and accumulation in FAP-positive tumor lesions while exhibiting minimal uptake in normal tissues, with the exception of the kidneys. This compound is particularly useful for tumor-related research applications, including imaging studies and the assessment of FAP's role in tumor biology. -
FAP Inhibitor
PNT6555 is a selective inhibitor of fibroblast activation protein-α (FAP), with notable antitumor activity. This compound is particularly valuable in the study of FAP-positive tumors, facilitating imaging applications that aid in tumor characterization and monitoring. Its specificity for FAP makes it a significant tool for cancer research, advancing the understanding of tumor microenvironments and potential therapeutic strategies. -
FAP Inhibitor
DOTAGA-FAP-2286-ALB is a selective inhibitor of fibroblast activation protein (FAP) with an IC50 value of 67.5 nM. This compound enhances tumor retention through its interaction with albumin, thereby prolonging blood circulation and increasing the stability of radiometal complexes such as 111In and 225Ac. DOTAGA-FAP-2286-ALB is of particular interest for research applications in radionuclide therapy (TRT) targeting FAP-positive solid tumors. -
FAP Radiotracer
NH2-UAMC1110 is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110, functioning as a precursor for the synthesis of FAP-targeted radiotracers. This compound is integral in producing the radiotracer FAPI-QS, known for its high tumor selectivity and dose-response, facilitating tumor diagnosis. NH2-UAMC1110 features an active amino group, allowing for covalent bonding with various molecules including bifunctional chelators like DOTA and DATA5m. It specifically binds to the FAP active site, inhibiting its serine protease activity, thereby blocking FAP-mediated tissue remodeling. Suitable for diagnostic imaging of tumors expressing FAP, NH2-UAMC1110 serves as a valuable tool in the study of FAP-related diseases such as fibrosis and arthritis. -
FAP Inhibitor
FAPI-2 is a quinoline-based inhibitor targeting fibroblast activation protein (FAP). It exhibits rapid tracer kinetics and is suitable for use as a PET tracer in cancer diagnosis, labeled with 68Ga. Notably, FAPI-2 does not require fasting preparation and remains effective regardless of blood glucose levels, making it a valuable tool for oncological research and imaging applications. -
FAP Inhibitor
FAP-IN-4 is a fibroblast activation protein (FAP) inhibitor that serves as an 18F-labeled PET tracer targeting FAP. This compound demonstrates significant potential in cancer research by facilitating the visualization of FAP-expressing tumors, thereby aiding in the understanding of tumor biology and treatment responses. It can be utilized in studies focused on tumor microenvironments and therapeutic interventions targeting FAP. -
FAP Inhibitor
SB03178 is a selective inhibitor of fibroblast activation protein-alpha (FAP). This compound demonstrates significant potential in cancer research, particularly in modulating tumor microenvironments and enhancing the efficacy of cancer therapies. Additionally, SB03178 can be conjugated with DOTA for further applications in targeted imaging and therapeutic strategies. -
FAP Inhibitor
FAP-IN-1 is a selective fibroblast activation protein (FAP) inhibitor that demonstrates potent activity with an IC50 value of 3.3 nM. This compound is valuable for investigating the role of FAP in the tumor microenvironment and its implications in cancer biology. FAP-IN-1 can be utilized in various research applications aimed at elucidating the mechanisms of tumor progression and the development of targeted therapeutic strategies. -
FAP Inhibitor
QI-18 is a potent inhibitor of fibroblast activation protein (FAP) with an IC50 of 0.50 nM, exhibiting 6.5-fold increased potency compared to UAMC-1110. Its high affinity makes QI-18 suitable for the development of radiotracers with enhanced tumor selectivity and dosage for tumor diagnosis and research applications. This compound plays a significant role in studies focusing on tumor microenvironments and potential therapeutic interventions targeting FAP. -
FAP-Targeting Peptide
3BP-4089 is a potent fibroblast activation protein (FAP)-targeting peptide designed for theranostic applications. This peptide effectively facilitates the targeting of tumor microenvironments, allowing for enhanced imaging and therapeutic strategies. Coupling 3BP-4089 with radionuclides supports its utility in tumor diagnosis and advanced cancer research. -
FAP Targeting Radioligand
DOTA-C1-FAP-2286 is a cysteic acid-modified radioligand that specifically targets fibroblast activation protein (FAP). With an IC50 of 127.64 nM, it binds competitively to FAP-expressing cells, allowing for targeted accumulation and expedited renal clearance. This compound is suitable for use as a PET/CT tracer in cancer research and can aid in the imaging of tumors with high FAP expression. -
FAP Inhibitor
FAPI-P8PN is a selective inhibitor of fibroblast activation protein (FAP), exhibiting an IC50 value of 3.6 nM. This compound is particularly useful for investigating FAP-overexpressing solid tumors, providing insights into tumor microenvironments and potential therapeutic approaches. Its targeted activity makes it a valuable tool in cancer research aimed at developing FAP-focused therapies. -
FAP Inhibitor
FAP-IN-8 is a selective inhibitor of fibroblast activation protein (FAP) and prolyl endopeptidase (PREP), exhibiting pIC50 values of 10.08 and 8.99 for these targets respectively. With IC50 values of 1 nM for FAP and 0.08 nM for PREP, FAP-IN-8 demonstrates potent inhibition that supports its utility in cancer research. This compound is valuable for studying tumor microenvironment interactions and the therapeutic targeting of cancer-associated fibroblasts. -
FAP Inhibitor
FAP-IN-7 is a selective inhibitor of fibroblast activation protein (FAP), a serine protease implicated in tumor progression and immune modulation. This compound effectively hinders FAP activity, contributing to the investigation of cancer-associated fibroblasts in the tumor microenvironment. FAP-IN-7 is valuable for research applications focused on understanding cancer biology, developing therapeutic strategies, and exploring the role of FAP in various disease states. -
FAP Radioligand
FAP6-19 is a radioligand targeting fibroblast activation protein (FAP) with a Kd of 18.2 nM. This compound selectively delivers therapeutic radioactive isotopes, such as 177Lu, directly to tumors that overexpress FAP in the microenvironment, enabling targeted destruction of malignant cells while preserving healthy tissues. FAP6-19 demonstrates high total cellular uptake and excellent intracellular retention in HT1080 cells. When labeled with 111In, it achieves favorable tumor/kidney and tumor/liver dose ratios in mouse models with 4T1 tumors. This reagent is valuable for research involving solid tumors that express FAP. -
FAP Inhibitor
DOTA-NI-FAPI-04 is a fibroblast activation protein (FAP) inhibitor with an IC50 of 7.44 nM, designed to enhance tumor uptake and retention using hypoxia-sensitive nitroimidazole groups. This compound forms stable complexes with metallic isotopes such as 68Ga and 177Lu through its DOTA moiety, serving as a foundation for the creation of radioactive probes ([68Ga]Ga/DOTA-NI-FAPI-04 and [177Lu]Lu/DOTA-NI-FAPI-04). DOTA-NI-FAPI-04 is valuable for research in cancer diagnostics, exploring the tumor microenvironment, and radionuclide therapy, particularly in the context of tumor stroma and hypoxic regions. -
FAP Inhibitor
3BP-3580 is a potent inhibitor of fibroblast activation protein (FAP), exhibiting a pIC50 of 8.6. This compound is relevant for cancer research, specifically in studies investigating tumor microenvironments and the role of FAP in cancer progression. Its ability to modulate FAP activity makes it a valuable tool for exploring therapeutic strategies in oncology. -
FAP Inhibitor
FAPI-X5 is a selective inhibitor of fibroblast activation protein (FAP) that binds to the catalytic domain, effectively disrupting its enzymatic activity through hydrogen bonding and π-π interactions. This compound exhibits significant cytostatic effects on glioblastoma tumors, resulting in reduced tumor growth without inducing regression. When radiolabeled with 68Ga, FAPI-X5 serves as a highly effective PET tracer, facilitating rapid tumor localization and high-contrast imaging in glioblastoma models. Additionally, FAPI-X5 can be labeled with 177Lu or 47Sc, functioning as a targeted radionuclide agent with extended tumor retention, making it valuable for glioblastoma research applications.
