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Catalog No.
Product Name
Application
Product Information
Citations
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Plasma Kallikrein Inhibitor
PKSI-527 is a highly selective plasma kallikrein inhibitor that targets the kallikrein-kinin system. It demonstrates significant potential in suppressing collagen-induced arthritis (CIA) by modulating inflammatory responses. PKSI-527 serves as a valuable tool for studying the role of plasma kallikrein in various pathological conditions and may aid in the development of therapeutic strategies for rheumatoid arthritis. -
Kallikrein Inhibitor
Feniralstat is a potent kallikrein inhibitor that exhibits an IC50 of 6.7 nM for human plasma kallikrein (pKal). This pyrazole derivative demonstrates selectivity, showing no inhibition on human KLKl, human FXIa, or human Factor XIIa, with IC50 values greater than 40 μM. Feniralstat is a valuable tool for investigating kallikrein-related pathways and may have implications in research focused on coagulation and inflammatory processes. -
Plasma Kallikrein Inhibitor
Berotralstat dihydrochloride is an orally active inhibitor of plasma kallikrein, a serine protease involved in the Bradykinin pathway. This compound has demonstrated efficacy in reducing brain edema and is under investigation for its therapeutic potential in glioblastoma and hereditary angioedema. Research applications include the study of inflammatory pathways and the modulation of vascular permeability in various disease states. -
Kallikrein Inhibitor
PPACK II diTFA is an irreversible inhibitor targeting glandular and plasma kallikreins. It demonstrates specificity in modulating kallikrein activity, making it a valuable tool for studies focused on coagulation, inflammation, and related pathways. This compound is essential for research exploring the physiological roles of kallikreins and their potential implications in various diseases. -
Plasma Kallikrein Inhibitor
Plasma kallikrein-IN-4 is a selective inhibitor of plasma kallikrein, exhibiting an IC50 of 0.016 μM against human plasma kallikrein. This compound effectively modulates the kallikrein-kinin system, contributing to its potential as a therapeutic agent in conditions associated with dysregulated bradykinin signaling. Plasma kallikrein-IN-4 is valuable for research applications focusing on cardiovascular diseases, inflammation, and pain signaling pathways. -
Kallikrein Inhibitor
LSP-249 is a potent plasma kallikrein inhibitor with an EC50 of less than 100 nM in cellular assays. This compound is currently being investigated for its therapeutic potential in treating angioedema. Its ability to modulate kallikrein activity makes it a valuable tool for research focused on vascular permeability and related disorders. -
Prekallikrein Inhibitor
Donidalorsen sodium is an antisense oligonucleotide that selectively targets prekallikrein (PKK). By binding to and promoting the degradation of PKK mRNA in the liver, Donidalorsen sodium effectively inhibits kallikrein activity and diminishes Bradykinin production. This reagent is particularly valuable for research applications related to hereditary angioedema. -
Kallikrein 5 Inhibitor
Eflumenibep alfa is a Kallikrein 5 inhibitor that exhibits anti-inflammatory properties. This fusion protein consists of human SPINK2 linked to the human IgG1 Fc fragment at the C-terminus, enabling it to effectively modulate inflammatory pathways. It is primarily used in research applications focused on inflammatory diseases and conditions related to kallikrein signaling. -
KLK6 Inhibitor
DKFZ-633 is a potent inhibitor of KLK6, exhibiting an IC50 of 250 nM against human KLK6. This compound covalently labels active KLK6 with high specificity, enabling the efficient pull-down and capture of endogenous KLK6 from cell-conditioned media. DKFZ-633 is an essential reagent for studying the role of KLK6 and its regulatory mechanisms, particularly in the context of head and neck cancer research. -
Plasma Kallikrein (pKal) Inhibitor
pKal-IN-1 is a selective inhibitor of plasma kallikrein (pKal), an enzyme involved in the kallikrein-kinin system, which plays a significant role in inflammatory processes. This compound has demonstrated the ability to modulate vascular permeability and inflammation, making it a valuable tool for studying diabetic macular edema and diabetic retinopathy. pKal-IN-1 can be utilized in various research applications aimed at understanding the therapeutic potential in treating these diabetes-related ocular conditions. -
Kallikrein Inhibitor
Ecallantide is a specific inhibitor of plasma kallikrein, effectively reducing the production of bradykinin. Its primary biological activity lies in the prevention of acute angioedema attacks, making it a valuable tool for research into conditions related to excessive bradykinin activity. Ecallantide is applicable in studies focusing on inflammatory responses and therapeutic interventions for angioedema disorders. -
Kallikrein Inhibitor
PPACK II is a potent irreversible inhibitor of glandular and plasma kallikreins, targeting their enzymatic activity. This compound is essential for studying the physiological roles of kallikreins in various biological processes, including inflammation and pain modulation. It is valuable for research applications focused on understanding kallikrein-related pathways and developing therapeutic strategies for associated diseases. -
Kallikrein-5 Inhibitor
GSK951 is a potent and selective inhibitor of Kallikrein-5 (KLK5), demonstrating an IC50 of 250 pM with over 100-fold selectivity against KLK7 and KLK14. This compound is designed for effective epidermal delivery and has been shown to reduce transepidermal water loss while decreasing pro-inflammatory cytokine expression. GSK951 is valuable for research applications in inflammation and immunology, particularly in studies related to Netherton syndrome. -
Kallikrein Inhibitor
Feniralstat hydrochloride is a potent inhibitor of kallikrein, with an IC50 value of 6.7 nM for human plasma kallikrein (pKal). This pyrazole derivative exhibits selectivity, showing no significant inhibition on human Kallikrein KLKl, FXIa, or Factor XIIa (IC50 values greater than 40 μM). Feniralstat is useful in research applications studying kallikrein's role in various biological processes and disease states, particularly in conditions associated with dysregulated kallikrein activity. -
FXIa/Kallikrein Inhibitor
FXIa/Plasma kallikrein-IN-1 is a potent inhibitor of coagulation factor XIa (FXIa) and plasma kallikrein, exhibiting Ki values of 187.70 nM and 151.6 nM, respectively. This compound serves as a valuable tool for investigating thromboembolic diseases and related disorders. Its selective inhibition of these targets can facilitate the exploration of pathological mechanisms and the development of therapeutic strategies for coagulopathies. -
Plasma Kallikrein Inhibitor
Plasma kallikrein-IN-3 is a potent inhibitor of plasma kallikrein, exhibiting an IC50 of 0.15 μM. This compound is relevant for research into hereditary angioedema, diabetic macular edema, and diabetic retinopathy. Its selective inhibition of plasma kallikrein supports investigations into related pathophysiological processes and therapeutic interventions. -
Protease Inhibitor
ONO-3307 is a potent protease inhibitor that acts competitively against a range of proteases, including trypsin, thrombin, plasma kallikrein, plasmin, pancreatic kallikrein, and chymotrypsin. This compound has demonstrated efficacy in alleviating endotoxin-induced experimental disseminated intravascular coagulation (DIC) in rat models. ONO-3307 is valuable for research into thrombosis and various protease-mediated diseases, providing insights into potential therapeutic strategies. -
PKK Inhibitor
Donidalorsen is an antisense oligonucleotide that selectively targets prekallikrein (PKK). By binding to and degrading PKK mRNA in the liver, Donidalorsen effectively inhibits kallikrein activity and reduces bradykinin production. This reagent is valuable for research focused on hereditary angioedema and related pathophysiological studies. -
KLK6 Inhibitor
DKFZ-251 is an inhibitor of the kininogenase-related peptidase KLK6, demonstrating an IC50 of 0.47 μM. It also shows inhibitory activity against KLK5 and KLK7 with IC50 values of 1.1 nM and 73 nM, respectively. This compound functions by transiently acylating the catalytic serine of KLK6, resulting in a stable acyl-enzyme complex that effectively inhibits enzymatic activity. DKFZ-251 serves as a phenotypic modulator, impacting cell proliferation and regulating epithelial-mesenchymal transition (EMT), making it a valuable tool in studies related to head and neck cancer. -
Kallikrein Inhibitor
KKI-5 is a selective inhibitor of tissue kallikrein, demonstrating significant activity in reducing breast cancer cell invasion. This compound is valuable for research into cancer biology and the mechanisms of metastasis, offering insights into potential therapeutic strategies targeting kallikrein-related pathways. -
LAG-3/MHCII and LAG-3/FGL1 PPI Inhibitor
SA-15-P is a potent inhibitor of the LAG-3/MHCII and LAG-3/FGL1 protein-protein interactions, with IC50 values of 4.21 μM and 6.52 μM, respectively. By disrupting these interactions, SA-15-P serves as a valuable tool in immunotherapy research, providing insights into immune regulation and the potential enhancement of anti-tumor responses. Its application facilitates the exploration of therapeutic strategies targeting LAG-3 in various disease contexts. -
LAG-3 Inhibitor
LAG-3-IN-2 is a selective inhibitor of LAG-3 (Lymphocyte Activation Gene 3), a key immune checkpoint involved in the regulation of T cell responses. By blocking LAG-3, this compound enhances T cell activation and proliferation, making it a valuable tool in immunological research. It is particularly relevant in studies focused on cancer immunotherapy and autoimmune diseases, where modulation of immune responses is critical. -
KRAS[G13C](ON) Inhibitor
RM-041 is a selective, orally active inhibitor targeting KRAS[G13C](ON), forming a covalent complex with both KRASG13C (ON) and Cyclophilin A. This compound effectively blocks the binding of RAS effector proteins through steric hindrance and irreversibly binds to Cys-13, leading to the inhibition of KRASG13C mutant cancer cell proliferation. RM-041 demonstrates significant regression of KRASG13C tumors in both cellular and xenograft tumor models and exhibits a synergistic effect in combination with upstream inhibitors, such as SHP2 inhibitors. It serves as a valuable research tool in studying non-small cell lung cancer. -
BCL6 Inhibitor
CCT374705 is a potent BCL6 inhibitor with an IC50 value of 4.8 nM, demonstrating significant antiproliferative effects in vitro. This compound effectively inhibits tumor growth in lymphoma xenograft mouse models, making it a valuable reagent for investigating BCL6-related pathways in cancer research and potential therapeutic applications. -
BCL6 Inhibitor
BCL6-IN-6 is a selective inhibitor targeting the transcriptional repressor B-cell lymphoma 6 (BCL6). It effectively disrupts the interaction between BCL6 and its corepressors, leading to the reactivation of BCL6 target genes in a dose-dependent manner. This compound is particularly relevant for studies focusing on diffuse large B-cell lymphoma (DLBCL) and related oncogenic pathways. -
BCL6 Inhibitor
GSK137 is a potent and selective inhibitor of B-cell lymphoma 6 (BCL6), acting primarily by disrupting the interaction between BCL6 and corepressors such as SMRT. This mechanism results in a reduction of germinal center B cells, making GSK137 a valuable tool for investigating autoimmune diseases, including systemic lupus erythematosus (SLE), and B-cell malignancies, such as diffuse large B-cell lymphoma. Its oral bioactivity aids in the exploration of therapeutic strategies targeting these conditions. -
BCL6 Inhibitor
BCL6-IN-11 is a potent BCL6 inhibitor that disrupts the interaction between BCL6 and its co-inhibitory proteins, such as NCOR1, with an IC50 value of 6 nM. This compound induces approximately 52% degradation of BCL6 at a concentration of 5 μM over 90 minutes, classifying it as a partial degrader. BCL6-IN-11 is valuable for research applications in studying lymphoma and the role of BCL6 in oncogenesis. -
BCL6 Inhibitor
WK692 is a potent inhibitor of BCL6, specifically targeting the BCL6 BTB/SMRT interaction. This compound demonstrates significant biological activity by effectively inhibiting the growth of diffuse large B-cell lymphoma cells. Furthermore, WK692 has been shown to synergize with EZH2 and PRMT5 inhibitors, making it a valuable tool for research into targeted cancer therapies and the mechanistic understanding of lymphoma progression. -
BCL6 Inhibitor
BCL6-IN-10 is a selective molecular glue inhibitor that targets the BTB domain of BCL6, exhibiting an IC50 of 4 nM. This compound demonstrates significant anti-proliferative activity in diffuse large B-cell lymphoma (DLBCL) cell lines, making it a valuable tool in cancer research. Its unique mechanism of action offers insights into therapeutic strategies for targeting BCL6-associated malignancies. -
BCL6 Inhibitor
SMRT peptide is a BCL6 inhibitor that functions by binding to the BTB domain of BCL6, thereby enhancing its transcriptional repression activity. This compound serves as a valuable tool for studying protein-protein interactions related to BCL6 function in various biological processes. Research applications include investigations into the role of BCL6 in cancer and other diseases where transcriptional regulation is critical. -
CD22 Inhibitor
GSC-718 is a synthetic sialoside and a potent inhibitor of CD22, exhibiting an IC50 value of 0.161 μM for mouse CD22. This compound is known to promote the proliferation of B cells and enhance antibody production. GSC-718 is particularly relevant for research applications involving B-cell lymphoma and autoimmune conditions such as rheumatoid arthritis. -
CD28-B7 Inhibitor
CD28-IN-2 is a selective inhibitor of the CD28-B7 interaction, demonstrating an IC50 of 22.4 μM and a Kd value of 24.1 μM. This compound effectively inhibits CD28-mediated immune activation and prevents T cell costimulation. CD28-IN-2 serves as a valuable tool in research investigating antitumor immunity and various immune-related disorders. -
CD272 Antibody Inhibitor
Radanstobart is a humanized monoclonal antibody that selectively inhibits CD272, a checkpoint protein involved in immune regulation. This antibody exhibits significant antitumor activity, making it valuable for cancer research and immunotherapy studies. It is classified as a human IgG4κ isotype, providing a robust platform for investigating immune responses and potential therapeutic approaches targeting the tumor microenvironment. -
B7.1-CD28 Interaction Inhibitor
B7/CD28 Interaction Inhibitor 1 is a selective inhibitor of the B7.1-CD28 interaction, exhibiting an IC50 of 50 nM. This compound disrupts T-cell costimulation, making it a valuable tool for research in immunology and cancer therapy. Its ability to modulate T-cell responses highlights its potential applications in studying immune regulation and developing immunotherapeutic strategies. -
CD28 Inhibitor
DDS5 is a selective CD28 inhibitor with an affinity (kd) of 175.57 µM, effectively disrupting the CD28-CD80 interaction with an IC50 value of 332 µM. This compound is instrumental in researching immune-mediated diseases, including inflammatory bowel disease and rheumatoid arthritis, enabling investigations into immune response modulation and therapeutic strategies. -
CD38 Inhibitor
CVN14 is a selective and potent inhibitor of CD38, exhibiting inhibitory activity with human and mouse IC50 values of 19 nM and 2.4 nM, respectively. This compound binds uncompetitively to CD38, forming a complex with ADPR and subsequently inhibiting its enzymatic activity. CVN14 is suitable for research applications focused on neurodegenerative diseases, providing insights into the role of CD38 in these conditions. -
CD38 Inhibitor
Luteolinidin chloride is a potent inhibitor of CD38, with a Ki value of 11.4 μM, and demonstrates significant antioxidant activity. This compound has shown to protect cardiac tissue from ischemia/reperfusion injury by preserving the functionality of endothelial nitric oxide synthase (eNOS) and preventing endothelial dysfunction. Additionally, Luteolinidin chloride acts as a competitive inhibitor of tyrosinase, with an IC50 of 3.7 μM, effectively blocking melanin production. This makes it a valuable reagent for research in cardiovascular protection and skin pigmentation studies. -
CD38 Inhibitor
CD38 Inhibitor 2 is a selective inhibitor of CD38 with an IC50 range of 0.01 to 0.1 μM. This compound demonstrates potent inhibition of CD38 enzymatic activity, making it a valuable tool for studies focused on NAD+ metabolism and immune regulation. Its applications extend to cancer research, immunology, and age-related studies, contributing to a better understanding of the role of CD38 in various biological processes. -
CD38 Inhibitor
Ara-F-NAD+ is an arabino analogue of NAD+ and functions as a potent, reversible, and slow-binding inhibitor of CD38 NADase. This compound effectively modulates NAD+ metabolism, making it a valuable tool for studying the role of CD38 in various biological processes. Ara-F-NAD+ has potential applications in research focused on immune regulation, cellular signaling, and metabolic disorders related to NAD+ homeostasis. -
CD38 Inhibitor
6-Alkyne-F-araNAD is an irreversible inhibitor of CD38, a critical enzyme involved in the regulation of cyclic ADP-ribose and NAD metabolism. This compound enhances the efficacy of fluorescent probes, such as SR101-F-araNMN, allowing for improved visualization of intracellular CD38 localization. It serves as a valuable tool in studies related to immune signaling and cellular response mechanisms. -
CD38 Hydrolase Inhibitor
CD38-IN-5 is a selective inhibitor of CD38 hydrolase, exhibiting an IC50 of 4.0 μM, while sparing CD38 cyclase activity. This compound is particularly effective in enhancing natural killer (NK) cell-mediated tumor cytotoxicity and promotes increased levels of NADH+ and IFNγ in activated peripheral blood mononuclear cells (PBMCs). CD38-IN-5 serves as a valuable tool for cancer research, facilitating the investigation of immune modulation and tumor interactions. -
CD38 Inhibitor
(E/Z)-CCR-11 is a selective inhibitor of CD38, exhibiting an IC50 value of 20.8 μM against CD38 cyclase. This compound effectively enhances cellular NAD+ levels and promotes the production of interferon γ. It is valuable for research applications focused on cellular metabolism and immune response modulation. -
HA-CD44 Interaction Inhibitor
HA-CD44 Interaction Inhibitor 2 is an inhibitor that targets the interaction between Hyaluronic acid (HA) and CD44. It exhibits antiproliferative effects on CD44-positive cancer cells, effectively disrupting cancer sphere integrity and decreasing cell viability in a dose-dependent manner. This compound is suitable for applications in tumor research aimed at understanding the role of CD44 in cancer progression. -
HA-CD44 Interaction Inhibitor
HA-CD44 Interaction Inhibitor 1 is a specific inhibitor of the interaction between hyaluronic acid (HA) and CD44. By disrupting this interaction, it demonstrates significant antiproliferative effects on CD44+ cancer cell lines. This compound is valuable for research aimed at understanding cancer progression and potential therapeutic strategies targeting CD44-mediated cellular processes. -
CD47 Inhibitor
Evorpacept is a high-affinity CD47 inhibitor designed to block the CD47-SIRPα immune checkpoint interaction. By binding to CD47, Evorpacept facilitates the inhibition of wild-type SIRPα binding, enhancing immune response against tumors. This reagent is particularly relevant for research applications focused on acute myeloid leukemia and other malignancies where CD47 plays a pivotal role in immune evasion. -
CD73 Inhibitor
CD73-IN-5 is a potent and selective small molecule inhibitor of CD73, exhibiting an IC50 value of 19 nM. This compound effectively interferes with the enzymatic activity of CD73, which plays a critical role in the production of adenosine in the tumor microenvironment. CD73-IN-5 is utilized in research applications exploring immunomodulation, cancer therapy, and the therapeutic potential of targeting adenosine signaling pathways. -
CD73 Inhibitor
CD73-IN-4 is a selective inhibitor of CD73, functioning through the blockade of adenosine production. With an IC50 of 2.6 nM against human CD73, it demonstrates significant potency in modulating immunosuppressive signals in the tumor microenvironment. This compound is valuable for investigating cancer immunology and exploring therapeutic strategies aimed at enhancing anti-tumor immune responses. -
CD73 Inhibitor
OP-5244 is a potent and orally active inhibitor of CD73, with an IC50 of 0.25 nM. By blocking adenosine production, OP-5244 effectively reverses immunosuppression, making it a valuable tool in cancer research. Its application can aid in the exploration of therapeutic strategies aimed at enhancing anti-tumor immunity. -
NTPDase1 Inhibitor
8-BuS-AMP is an inhibitor of NTPDase1, CD73, and CD39, demonstrating an IC50 of 35 μM and a Ki of 0.292 μM for human NTPDase1, alongside Ki values of 1.19 μM for CD73 and 0.847 μM for CD39. This compound interacts with the substrate-binding sites of NTPDase1 and CD73, effectively preventing the conversion of ATP and AMP to adenosine, which promotes the activation and proliferation of human peripheral T lymphocytes. 8-BuS-AMP exhibits robust enzymatic hydrolysis resistance and metabolic stability, and it has no activity against P2Y1 and P2Y12 receptors. This reagent is suitable for investigations into purinergic signaling pathways and cancer research. -
CD73 Inhibitor
ORIC-533 is a selective, orally active inhibitor of CD73 that operates through an AMP-competitive mechanism, demonstrating potent inhibition of adenosine production with a sub-nanomolar affinity (Ka 0.03 nM). This compound has shown significant promise in the context of multiple myeloma, as it enhances the cytotoxic activity of the immune system against tumor cells by reversing immunosuppression, inducing immunogenic cell death, and activating various immune cells including dendritic cells, T cells, and NK cells, while exhibiting minimal toxicity to normal cells. Furthermore, combined administration of ORIC-533 with daratumumab effectively increases intratumoral CD8+ T cell infiltration and substantially inhibits tumor growth in preclinical models.
