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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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 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. -
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-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. -
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. -
Galectin-8N Inhibitor
Galectin-8-IN-2 is a selective inhibitor of galectin-8N, a member of the galectin family implicated in various biological processes. This compound exhibits significant inhibitory activity, making it a valuable tool for investigating galectin-mediated pathways and their roles in disease mechanisms. It is particularly useful for research focused on cancer, inflammation, and immune response modulation. -
Galectin 4 Inhibitor
Galectin-4-IN-2 is a potent inhibitor of galectin-4C, exhibiting a dissociation constant of 1.6 mM. This compound is valuable for studies investigating the role of galectin-4 in various biological processes, including cell adhesion, immune response, and cancer biology. Research applications include elucidating the mechanisms of galectin-mediated pathways and exploring therapeutic strategies targeting galectin proteins in disease models. -
Galectin-3 Inhibitor
Galectin-3-IN-4 is a selective carboxamide inhibitor targeting galectin-3, with an IC50 of 21 nM for human galectin-3 and 167 nM for mouse galectin-3. This compound demonstrates significant selectivity, showing much higher IC50 values of 1580 nM and 2750 nM for human galectin-1 and galectin-9, respectively. Galectin-3-IN-4 is orally bioavailable, making it a valuable tool for research into the role of galectin-3 in various biological processes, including cancer, inflammation, and fibrosis. -
Gal-3 Inhibitor
Galectin-3-IN-2 is a potent multivalent inhibitor of galectin-3 (Gal-3), exhibiting an IC50 value of 8.3 μM. Galectin-3 is involved in various cancer-related metabolic processes, making this compound valuable for research into cancer biology and therapeutic development. Its application as a Gal-3 inhibitor allows for the exploration of its role in tumor progression, metastasis, and immune response modulation. -
Galectin-3 Inhibitor
Galectin-3-IN-6 is a potent inhibitor of galectin-3, displaying an IC50 of 12 nM against human galectin-3 and 12.6 nM against the mutant murine galectin-3 (V160A), along with a Kd of 13 nM. This compound effectively reduces markers of liver fibrosis, including type I collagen and α-smooth muscle actin, in murine models of acute liver injury and fibrosis. Galectin-3-IN-6 serves as a valuable tool for investigating the mechanisms and potential therapies for acute liver injury and related fibrotic conditions. -
Gal-3 Inhibitor
Galectin-3-IN-3 is a selective inhibitor of galectin-3, exhibiting potent activity with IC50 values of 11 nM for mouse galectin-3 and 84 nM for human galectin-3. This compound serves as a valuable tool for studying the role of galectin-3 in various biological processes, including tumor progression, inflammation, and fibrosis. Its oral bioavailability allows for convenient administration in preclinical models, facilitating research in therapeutic applications targeting galectin-3-related pathologies. -
Galectin-1 Inhibitor
GB1490 is a potent galectin-1 inhibitor, exhibiting a Kd value of 0.4 μM. Additionally, it shows inhibitory activity against galectin-3 with a Kd of 2.7 μM. This compound is primarily utilized in research to investigate the role of galectins in various biological processes, including cancer progression and immune response modulation. Its selectivity and potency make it a valuable tool in studies aimed at understanding galectin-related pathways. -
Galectin-8N Inhibitor
Galectin-8N-IN-2 is a selective inhibitor of Galectin-8N, exhibiting a Ki value of 74 µM. This compound is essential for investigating the role of Galectin-8N in biological processes, particularly in modulating cell adhesion, immune responses, and tumor progression. Its inhibitory action facilitates research into therapeutic strategies targeting galectins in cancer and autoimmune diseases. -
RIG-I Inhibitor
RIG012 is a potent inhibitor of RIG-I with an IC50 of 0.71 μM, as determined by the NADH-coupled ATPase assay. It effectively suppresses the expression of interferon beta (IFN-β) and the interferon-stimulated gene hRsad2. RIG012 is valuable for research applications focusing on the modulation of innate immune responses and the study of viral infections. -
IRF5 Inhibitor
YE6144 is a selective interferon regulatory factor 5 (IRF5) inhibitor. It exhibits significant biological activity by suppressing disease progression and is particularly effective for maintaining remission in murine models of systemic lupus erythematosus (SLE). This compound serves as a valuable tool for researchers investigating the mechanisms of SLE and the role of IRF5 in autoimmune diseases. -
Mi-2β-targeted Inhibitor
Z36-MP5 is a targeted inhibitor of Mi-2β, exhibiting an IC50 value of 0.082 μM. This compound effectively reduces Mi-2β ATPase activity, leading to the reactivation of interferon-stimulated gene (ISG) transcription. Additionally, Z36-MP5 is known to enhance T-cell-mediated cytotoxicity, making it a valuable tool for research in immunology and potential therapeutic applications in cancer and viral infections. -
SLCl5A4 Inhibitor
IFNα-IN-1 is an SLC5A4 inhibitor that specifically targets and inhibits the production of interferon-alpha (IFN-α). Its primary biological activity is to modulate the inflammatory response by reducing IFN-α levels. This reagent is suitable for research applications focused on studying inflammation and related disease mechanisms. -
VISTA Inhibitor
VISTA-IN-3 is a potent small molecule inhibitor of the VISTA pathway, exhibiting a KD value of 0.49 μM. It effectively induces the release of IFN-γ cytokines, thereby enhancing immune responses. Additionally, VISTA-IN-3 demonstrates synergistic effects when combined with PD-L1 antibodies, making it a valuable tool for cancer immunotherapy research. -
IFN alpha-IFNAR Inhibitor
IFN alpha-IFNAR-IN-1 is a small-molecule inhibitor that specifically targets the interaction between interferon-alpha (IFN-α) and its receptor, IFNAR. This compound effectively inhibits IFN-α responses induced by modified Vaccinia virus Ankara (MVA) in murine bone marrow-derived plasmacytoid dendritic cell (pDC) cultures, exhibiting an IC50 of 2-8 μM. It serves as a valuable tool for studying the immune response modulation in various infectious and inflammatory conditions. -
IFNβ inhibitor
StA-IFN-1 is a selective inhibitor of type I interferon (IFN), specifically targeting the activation of IFNβ with an IC50 of 4.1 μM. This compound is utilized in research exploring the roles of IFNβ in immune responses and associated pathologies. Its inhibitory properties make it a valuable reagent for studying the modulation of inflammatory processes and therapeutic strategies in various disease models. -
IRF5 Inhibitor
YE6144 free base is a selective inhibitor of interferon regulatory factor 5 (IRF5). It effectively suppresses disease progression and is particularly beneficial for maintaining remission in preclinical models of systemic lupus erythematosus (SLE). This compound serves as a valuable tool for researchers investigating the role of IRF5 in autoimmune disorders and potential therapeutic strategies for SLE. -
IRF3 Inhibitor
Sim-9 is a covalent allosteric inhibitor targeting interferon regulatory factor 3 (IRF3). By binding covalently to the Cys222 residue, Sim-9 induces a conformational change that inhibits interactions between IRF3 and key signaling partners such as TRIF, MAVS, and STING, ultimately blocking homodimerization and the type I interferon response. This compound demonstrates significant anti-inflammatory and organ-protective effects in mouse models of sepsis and acute pancreatitis, making it a valuable tool for research focused on inflammatory diseases. -
IKZF2 Selective and orally Inhibitor
PVTX-405 is a selective, orally bioavailable inhibitor targeting IKZF2, designed as a molecular glue degrader. With a DC50 of 0.7 nM and a Dmax of 91%, it enhances degradation efficiency while minimizing off-target effects, exhibiting an IC50 of 48 µM for hERG inhibition. PVTX-405 demonstrates significant antitumor activity by inhibiting the growth of MC38 tumors and shows improved efficacy when combined with immune checkpoint therapies, such as anti-PD1 or anti-LAG3, in mouse models. -
IDE/NLRP3 Inhibitor
ML345 is a selective inhibitor of insulin-degrading enzyme (IDE) and NLRP3, exhibiting an IC50 of 188 nM for IDE. By targeting the Cys819 residue, ML345 effectively inhibits IDE activity, while it binds non-covalently to NLRP3, modulating its function. This compound is known to inhibit the release of inflammatory cytokines such as IL-1β and IL-6, demonstrating significant anti-inflammatory properties. Additionally, ML345 has been shown to provide protective effects against miscarriage, making it a valuable tool for research in inflammation and reproductive health. -
KLK5 Inhibitor
Kallikrein 5-IN-2 is a selective inhibitor of Kallikrein 5 (KLK5), exhibiting a pIC50 of 7.1. This compound demonstrates the ability to regulate epidermal shedding, potentially alleviating related inflammation and pruritus. Kallikrein 5-IN-2 serves as a valuable tool in research focused on dermatological conditions and the modulation of skin barrier function. -
Plasma Kallikrein Inhibitor
Sebetralstat is a selective inhibitor of plasma kallikrein, a serine protease involved in the kallikrein-kinin system. This compound demonstrates significant activity in modulating bradykinin levels, making it relevant for investigating metabolic diseases and conditions associated with dysregulated kallikrein activity. Its ability to inhibit plasma kallikrein positions Sebetralstat as a valuable tool for research into therapeutic strategies for associated pathologies. -
Coagulation Factor XII/Kallikrein Inhibitor
D-Pro-Phe-Arg-Chloromethylketone is a selective inhibitor of coagulation factor XII and plasma kallikrein. This compound is essential for studying the mechanisms of thrombosis and inflammation, making it a valuable tool for research in cardiovascular diseases and related fields. Its ability to inhibit these factors can provide insights into the regulation of hemostasis and the inflammatory response. -
Plasma Kallikrein Inhibitor
KVD-001 is a potent inhibitor of plasma kallikrein, a serine protease involved in the kallikrein-kinin system. This compound demonstrates significant biological activity by modulating vascular permeability and inflammatory responses. KVD-001 is applicable in research focused on diabetic macular edema, providing valuable insights into therapeutic interventions for ocular diseases. -
Tissue Kallikrein Inhibitor
FE-999024 is a selective inhibitor of tissue kallikrein, a serine protease involved in various physiological processes. This compound has demonstrated the ability to reduce cancer cell invasion by up to 39% and to decrease eosinophilia in models of allergic inflammation. FE-999024 serves as a valuable tool in research focused on cancer, inflammation, and immunology, contributing to a deeper understanding of these biological pathways. -
Plasma Kallikrein Inhibitor
Berotralstat is an orally active plasma kallikrein inhibitor that demonstrates significant potential in the modulation of vascular permeability. By inhibiting plasma kallikrein, Berotralstat has been shown to reduce brain edema, making it a valuable candidate for research in glioblastoma and hereditary angioedema. Its application in these areas may contribute to improved therapeutic strategies for conditions characterized by excessive vascular leakage and inflammation.
