Catalog No.
Product Name
Application
Product Information
Citations
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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. -
FEN1 Inhibitor
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. -
FLAP Inhibitor
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 Inhibitor
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. -
FLAP Inhibitor
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. -
CRBN Degrader
WDR5 Degrader-1 is a cereblon (CRBN)-recruiting compound designed to selectively induce degradation of the WDR5 protein. This degrader effectively targets WDR5 while sparing the CRBN neo-substrate IKZF1, facilitating precise manipulation of WDR5 levels in cellular systems. It is a valuable tool for investigating the biological roles of WDR5 in transcriptional regulation and potential therapeutic strategies in diseases associated with dysregulated WDR5 expression. -
A2AR Antagonist
A2AR-antagonist-1 is a selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 29 nM. This compound demonstrates significant anti-tumor activity and maintains metabolic stability in mouse liver microsomes (t1/2 = 86.1 min). Additionally, A2AR-antagonist-1 activates T cells by inhibiting immunosuppressive molecules such as LAG-3 and TIM-3, while promoting the expression of effector molecules including GZMB, IFNG, and IL-2, making it a valuable tool in cancer immunotherapy research. -
SIK2/3 Inhibitor
SIK2/3-IN-2 is a potent inhibitor of salt-inducible kinases 2 and 3 (SIK2 and SIK3), with IC50 values of 65 nM and 14 nM, respectively. Additionally, it acts as a p21-activated protein kinase (PAK) 1 inhibitor with a Ki of 20.7 nM. This compound is valuable for investigating hyperproliferative diseases and cancer, particularly in studies related to Paclitaxel-resistant ovarian cancer. -
Anti-Inflammatory Agent
Cholesterol sulfate is a naturally occurring cholesterol derivative that functions as a DOCK2 inhibitor, exhibiting IC50 values of 2 μM for mouse targets and 2.9 μM for human targets. This compound shows significant anti-inflammatory activity by limiting neutrophil infiltration and mitigating intestinal inflammation and damage. Additionally, it activates protein kinase C (PKC), facilitating squamous cell differentiation and inhibiting skin carcinogenesis. Cholesterol sulfate is relevant for research applications in conditions such as actinic keratitis, ulcerative colitis, and skin cancer, and it plays a role in regulating cholesterol homeostasis and cellular metabolism via the AMPK-Sirt1 pathway. -
CypD Inhibitor
CypD-IN-5 is a selective inhibitor of cyclophilin D (CypD), a key regulator of mitochondrial permeability transition. This compound demonstrates significant potential in modulating mitochondrial function and may be particularly useful in studying neurodegenerative diseases such as Alzheimer's disease. Its application in research focuses on understanding the role of CypD in cellular stress responses and the underlying mechanisms of neurodegeneration. -
Anti-CLDN18/CD3E Antibody
Emaretamig is a humanized IgG1κ monoclonal antibody that selectively targets CLDN18 and CD3E. This compound exhibits significant anti-tumor efficacy and is primarily employed in research on gastric and pancreatic cancers. Its mechanism of action facilitates T-cell engagement with tumor cells, enhancing immune-mediated responses against malignancies expressing these antigens. -
Anti CLDN18.2 & CD3E Antibody
Lumivatamig is a bispecific antibody designed to target CLDN18.2 and CD3E, facilitating T-cell-mediated cytotoxicity against CLDN18.2-expressing tumors. This dimer-type H-γ1_L-κ-scFvhl antibody is employed in cancer immunotherapy research to enhance anti-tumor immune responses. Its ability to bridge tumor cells and T cells may contribute to improved therapeutic outcomes in clinical applications targeting gastric and pancreatic cancers. -
FLAP/sEH Inhibitor
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. -
FEN1 Inhibitor
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 Inhibitor
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 Inhibitor
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 Inhibitor
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 Inhibitor
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. -
FLAP Inhibitor
(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. -
FLAP Inhibitor
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. -
FLAP Inhibitor
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. -
Leukotriene Biosynthesis Inhibitor
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. -
FLAP Inhibitor
AM103 (free acid) is a selective inhibitor of 5-lipoxygenase activating protein (FLAP), effectively blocking the initial step of the leukotriene biosynthetic pathway. This compound demonstrates significant inhibition of leukotriene B4 and cysteinyl leukotriene production, exhibiting notable anti-inflammatory properties in murine models of chronic lung inflammation. Additionally, AM103 (free acid) has been shown to enhance survival in mice challenged with platelet-activating factor, making it a valuable tool for research into respiratory disorders, including asthma. -
FLAP Antagonist
ALR-6 is a selective antagonist of the 5-lipoxygenase-activating protein (FLAP), known for its anti-inflammatory properties. This compound effectively inhibits the formation of 5-LOX products by more than 80% in pro-inflammatory M1 monocyte-derived macrophages (MDM), while demonstrating minimal direct inhibition of 5-LOX activity. ALR-6 is valuable for research applications aimed at exploring inflammatory pathways and potential therapeutic interventions in inflammatory diseases. -
FLAP Inhibitor
FLAP-IN-1 is a potent 5-lipoxygenase-activating protein (FLAP) inhibitor, exhibiting an IC50 value of 654 nM. This compound is useful for investigating the role of FLAP in inflammatory pathways and its potential implications in cardiovascular disease research. Researchers can leverage FLAP-IN-1 to explore therapeutic strategies targeting leukotriene biosynthesis and related conditions. -
FEN1 Inhibitor
FEN1-IN-8 is a selective inhibitor of flap endonuclease 1 (FEN1), exhibiting an IC50 of less than 100 nM for FEN1 and a range of 100 nM to 1 μM for exonuclease 1 (EXO1). This compound serves as a valuable tool for studying the role of FEN1 in colorectal and gastric cancers, providing insights into tumor biology and potential therapeutic pathways. FEN1-IN-8 is suitable for research applications focused on understanding DNA repair mechanisms and their implications in cancer progression. -
FLAP Antagonist
ALR-27 is a selective antagonist of the 5-lipoxygenase activating protein (FLAP), exhibiting significant anti-inflammatory properties. This compound effectively inhibits the formation of 5-LOX products by more than 80% in pro-inflammatory M1 macrophage-derived macrophages (M1-MDM), without directly inhibiting 5-LOX activity. Additionally, ALR-27 reduces the production of prostaglandins and leukotrienes in neutrophils while promoting the synthesis of specialized pro-resolving mediators in distinct human macrophage phenotypes. These characteristics make ALR-27 valuable for research in inflammation and immune response modulation. -
Galectin-3 Inhibitor
Olitigaltin is a synthetic inhibitor of galectin-3, demonstrating a high binding affinity with a Kd value of 68 nM. This compound exhibits significantly lower affinity for galectin-1 and galectin-7, with Kd values of 0.22 μM and 38 μM, respectively. Olitigaltin is valuable for research applications investigating the role of galectin-3 in various biological processes, including inflammation, fibrosis, and cancer progression. -
Galectin Inhibitor
Thiodigalactoside is a potent inhibitor of galectins, specifically targeting GAL1 and GAL3 with Kd values of 24 μM and 49 μM, respectively. As a non-metabolizable disaccharide, it demonstrates significant anti-inflammatory and anti-cancer properties. Additionally, Thiodigalactoside has been shown to effectively reduce body weight gain in diet-induced obese rat models, making it a valuable tool for studying metabolic disorders and galectin-related diseases. -
Gal-3 Inhibitor
Selvigaltin (GB1211) is an orally active inhibitor of galectin-3, exhibiting a potent IC50 of 12 nM in rabbit models. This compound demonstrates significant anti-tumor activity by effectively reducing galectin-3 levels in the liver, which leads to decreased biomarkers associated with liver function, inflammation, and fibrosis. Additionally, Selvigaltin downregulates the expression of key inflammatory and fibrotic markers, such as IL6, TGFβ3, SNAI2, and collagen, while also restoring T-cell activity, thereby impeding tumor growth and metastasis. It serves as a valuable tool for research into therapeutic strategies targeting galectin-3 related disorders. -
Galectin-3 Inhibitor
β-Lactose is a disaccharide that serves as an inhibitor of galectin-3, a protein involved in various biological processes, including cell adhesion and immune response. Its ability to modulate galectin-3 activity makes it a valuable tool in research pertaining to cancer, inflammation, and fibrosis. Additionally, β-lactose can be utilized as a substrate in studies of lactose metabolism and as a model compound for investigating carbohydrate-protein interactions. -
Galectin-3 Antagonist
Galectin-3 antagonist 1 is a specific inhibitor of Galectin-3, exhibiting a Kd value of 5.3 μM. This compound also demonstrates binding affinities to other galectins, with Kd values of 250 μM for Gal-4N, 18 μM for Gal-4C, and 450 μM for Gal-8C. It serves as a valuable tool for investigating the role of Galectin-3 in various biological processes and its implications in disease states, making it suitable for research in cancer, inflammation, and fibrosis. -
immunosuppressive
4,5-Dibromo-2-pyrrolic acid is an immunosuppressive compound that acts by inhibiting the proliferative response of splenocytes. This compound has been shown to significantly reduce the activation of immune cells in response to suboptimal concentrations of the mitogen concanavalin A (Con A). Its primary applications include research in immune regulation and the study of immunosuppressive mechanisms. -
galectin-8N Inhibitor
Galectin-8N-IN-1 is a selective inhibitor targeting galectin-8N, exhibiting a Kd value of 1.8 μM. This compound serves as a valuable ligand for galectin-8N studies and plays a critical role in researching immune system mechanisms. Its potent inhibition of galectin-8N makes it an essential tool for exploring immune modulation and related biochemical pathways. -
Galectin-1 Inhibitor
GB1908 is a selective oral inhibitor of galectin-1, demonstrating Ki values of 57 nM and 72 nM for human and mouse galectin-1, respectively. This compound exhibits over 50-fold selectivity for galectin-1 compared to galectin-3. GB1908 serves as a valuable tool in the investigation of lung cancer and related therapeutic strategies, facilitating research into the role of galectin-1 in tumor progression and immune modulation. -
Click Chemistry
Thiobis-β-Galactose-propyne serves as a versatile click chemistry reagent with an alkyne functional group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions. Primarily, it acts as a multivalent inhibitor of galectin-3 (Gal-3), a protein implicated in various metabolic processes associated with cancer progression. This compound is suitable for applications in biochemical research focused on galectin-3-related pathways and provides a valuable tool for the development of targeted therapeutic strategies. -
Galectin-1 Inhibitor
DB21 is a Galectin-1 antagonist that functions as an allosteric inhibitor of galectin-1 binding to cell surface glycans. This dibenzofuran-conjugated peptidomimetic demonstrates significant inhibition of angiogenesis and tumor growth in models of melanoma, lung adenocarcinoma, and ovarian cancer. Its ability to disrupt galectin-1 interactions positions DB21 as a valuable tool for cancer research and therapeutic development. -
Galectin-3/Galectin-8C Inhibitor
Galectin-3/Galectin-8-IN-1 is a dual inhibitor targeting the C-terminal domains of Galectin-3 and Galectin-8, exhibiting Kd values of 4.12 μM and 6.04 μM, respectively. This compound effectively hinders migration in MRC-5 lung fibroblast cells, highlighting its potential role in modulating cellular processes. Galectin-3/Galectin-8-IN-1 is applicable in cancer research and studies focusing on tissue fibrosis, offering insights into therapeutic strategies for these conditions. -
Galectin-3 Inhibitor
GB2095 is a selective inhibitor of galectin-3, demonstrating strong binding affinity with human (KD = 0.036 μM) and mouse (KD = 0.35 μM) variants. This compound exhibits significant anti-tumor activity in syngeneic mouse models, specifically for breast and melanoma cancers. GB2095 is valuable for research applications aimed at understanding the role of galectin-3 in cancer progression and therapeutic interventions. -
Galectin 4C Inhibitor
Galectin-4-IN-3 is a selective inhibitor of Galectin 4C, exhibiting a Kd of 160 μM. This compound is valuable for studies investigating the role of Galectins in cell-cell adhesion, immune response regulation, and cancer progression. Researchers can utilize Galectin-4-IN-3 to explore potential therapeutic strategies targeting Galectin-mediated pathways in various disease contexts.
