Immunology & Inflammation

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-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.

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.

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-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.

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.

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.

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.

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.

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.

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.

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.

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.

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-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.

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.

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.

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.

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.

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.

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.

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.

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-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.

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-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.

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.

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.

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.

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-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-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.

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.

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.

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.

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.

FEN1-IN-4 is a selective inhibitor of human flap endonuclease-1 (hFEN1), targeting the enzyme's crucial role in DNA replication and repair. This compound demonstrates significant biological activity by obstructing hFEN1's enzymatic function, which is essential for maintaining genomic stability. FEN1-IN-4 is valuable for research applications in cancer biology and the study of DNA repair mechanisms, providing insights into potential therapeutic strategies for related diseases.

BRP-7 is a highly selective FLAP inhibitor with an IC50 of 0.31 μM. By targeting the 5-lipoxygenase activating protein (FLAP), BRP-7 effectively interrupts the co-localization of FLAP and 5-lipoxygenase, inhibiting the transfer of arachidonic acid and consequently reducing leukotriene production (IC₅₀ = 0.15 μM). It does not inhibit cyclooxygenase (COX-1/COX-2) or microsomal prostaglandin E₂ synthase-1 (mPGES-1), and maintains cell viability. BRP-7 has demonstrated significant anti-inflammatory properties in rodent models of pleurisy and peritonitis, making it a valuable tool for investigating inflammatory diseases.

FEN1-IN-2 is a selective inhibitor of flap endonuclease 1 (FEN1), demonstrating an IC50 of 3 nM. It exhibits significantly lower activity against XPG, with an IC50 of 226 nM. This compound is valuable for investigating FEN1's role in DNA repair processes and its potential implications in cancer research. Researchers can utilize FEN1-IN-2 to study mechanisms of cellular response to DNA damage and identify therapeutic strategies targeting FEN1-related pathways.

Atuliflapon (AZD5718) is a potent, orally active inhibitor of FLAP (5-Lipoxygenase Activating Protein), exhibiting an IC50 of 2 nM. This compound is primarily utilized in research related to inflammatory processes, particularly in the context of coronary artery disease. Its selective inhibition of FLAP contributes to the regulation of leukotriene biosynthesis, making it a valuable tool for investigating therapeutic strategies for cardiovascular conditions.

Diflapolin is a potent dual inhibitor of 5-lipoxygenase-activating protein (FLAP) and soluble epoxide hydrolase (sEH), demonstrating significant anti-inflammatory effects and high target selectivity. It effectively inhibits the formation of 5-LOX products in human monocytes and neutrophils with IC50 values of 30 nM and 170 nM, respectively, while also inhibiting isolated sEH with an IC50 of 20 nM. This compound is valuable for research into inflammatory pathways and related therapeutic interventions.

MSC778 is a potent and orally bioavailable inhibitor of flap endonuclease 1 (FEN1), exhibiting an IC50 of 3 nM and a KD of 2.9 nM. It demonstrates significant selectivity with 145-fold, 516-fold, and 65-fold greater inhibition over EXO1, GEN1, and XPG, respectively. MSC778 preferentially induces apoptosis in BRCA2-deficient cells and enhances the efficacy of Niraparib in tumor stasis within BRCA2 knockout DLD-1 mouse xenografts. This compound is valuable for research focused on colorectal cancer.

FEN1-IN-7 is a selective inhibitor of Flap endonuclease-1 (FEN1), with an IC50 of 18 nM, crucial for DNA repair in mammalian cells. In addition, it exhibits activity against xeroderma pigmentosum G (XPG) with an IC50 of 3.04 μM. FEN1-IN-7 enhances the sensitivity of cancer cells to DNA alkylating and methylating agents, making it a valuable tool for research in cancer therapy and DNA damage response mechanisms.

FEN1-IN-5 is a potent inhibitor of Flap endonuclease-1 (FEN1) with an IC50 of 12 nM. FEN1 plays a crucial role in DNA repair processes, particularly in the maturation of Okazaki fragments during DNA replication. This compound serves as a valuable tool in research applications aimed at dissecting the mechanisms of DNA repair and exploring potential therapeutic targets for conditions associated with FEN1 dysfunction.

FEN1-IN-6 is a potent inhibitor of Flap endonuclease-1 (FEN1), with an IC50 of 10 nM. This compound plays a significant role in cellular mechanisms for DNA damage repair, enhancing research into DNA repair processes. Additionally, FEN1-IN-6 exhibits activity against the related endonuclease xeroderma pigmentosum G (XPG) with an IC50 of 23 nM, making it a valuable tool for studying nucleic acid metabolism and repair pathways.

FEN1-IN-3 is a selective inhibitor of human flap endonuclease-1 (hFEN1), a crucial enzyme involved in DNA replication and repair. With an EC50 value of 6.8 µM, FEN1-IN-3 effectively stabilizes hFEN1, making it a valuable tool for studying DNA metabolic processes. This compound is suitable for research applications focused on cancer biology, gene expression regulation, and the exploration of therapeutic strategies targeting DNA repair mechanisms.

(S)-BI 665915 is a potent FLAP (5-lipoxygenase-activating protein) inhibitor with an IC50 of 1.7 nM, effectively targeting FLAP binding. This compound demonstrates functional inhibition of FLAP in human whole blood with an IC50 of 45 nM and exhibits favorable drug metabolism and pharmacokinetics (DMPK) across species. (S)-BI 665915 provides dose-dependent inhibition of leukotriene B4 (LTB4) production, making it a valuable tool for research into inflammatory responses and related biological pathways.

BI 665915 is a potent oral inhibitor of the 5-lipoxygenase-activating protein (FLAP). By inhibiting FLAP, this compound effectively blocks the biosynthesis of leukotriene B4 (LTB4), making it a valuable tool for exploring inflammatory pathways. BI 665915 has potential applications in research related to various inflammatory diseases, including those affecting the respiratory and cardiovascular systems.

L-669083 is a potent FLAP (5-lipoxygenase-activating protein) inhibitor that specifically targets leukotriene biosynthesis. It is structurally derived from a combination of indole and quinoline, showcasing significant activity in disrupting leukotriene production. Research applications include studying inflammatory responses and evaluating the role of leukotrienes in various disease models, making L-669083 a valuable tool in pharmacological investigations related to inflammation and related pathologies.

L 689037 is a potent leukotriene biosynthesis inhibitor that targets the 5-lipoxygenase-activating protein (FLAP). This compound effectively disrupts the synthesis of leukotrienes, which are mediators of inflammation. L 689037 is valuable for research applications related to asthma and inflammatory bowel disease, aiding in the investigation of therapeutic strategies to mitigate these inflammatory conditions.