Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Substrate for Kallikrein
D-Val-Leu-Arg-pNA acetate serves as a substrate for the serine protease kallikrein. It enables the assessment of kallikrein activity through the release of p-nitroaniline upon peptide cleavage. This compound is valuable for research applications focused on the role of kallikrein in various physiological and pathological processes, providing insights into its functions in inflammation and fluid regulation. -
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. -
Prekallikrein synthesis reducer
Onvuzosiran is a small interfering RNA (siRNA) that effectively reduces the synthesis of prekallikrein, a key component in the contact activation pathway of blood coagulation. By targeting and silencing the gene responsible for prekallikrein production, Onvuzosiran plays a crucial role in research focused on thrombosis, inflammatory responses, and related cardiovascular disorders. This reagent is essential for studies investigating the modulation of the coagulation cascade and the development of novel therapeutic strategies. -
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. -
Target Protein Ligand
LAG-3 degrader 1 is a PROTAC target protein ligand designed for the synthesis of PROTACs targeting LAG-3. This compound facilitates the targeted degradation of LAG-3, demonstrating significant anti-tumor activity. It serves as a valuable tool in cancer research, allowing for the exploration of LAG-3 modulation in therapeutic applications. -
LAG-3 Ligand
LAG-3 biner 1 is a small molecule ligand that specifically targets the immune checkpoint lymphocyte activation gene 3 (LAG-3), exhibiting a Kd of 1.23 μM. This compound plays a significant role in modulating immune responses and is valuable for research applications focused on cancer diagnostics and the exploration of immune regulation involving LAG-3. -
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. -
LAG-3 D1 Ligand
Z3071585108 is a small molecule inhibitor of the LAG-3 D1 domain, exhibiting Kd values of 59.2 μM and 56.1 μM through MST-TRIC channel and spectral shift detection, respectively. This compound partially inhibits the interaction between LAG-3 and MHC class II molecules, with an EC₅₀ value of 42.9 μM. Z3071585108 is valuable for research on small molecule immunotherapies targeting the LAG-3 pathway, contributing to the understanding of immune modulation in various diseases. -
Bioactive Peptide
OVA-T4 Peptide (SIITFEKL) is a bioactive peptide variant of the ovalbumin epitope (OVA (257-264)), known for its binding to H-2Kb MHC class I molecules. This peptide exhibits comparable binding strength to H-2Kb but demonstrates significantly reduced affinity for the OT-I TCR. OVA-T4 Peptide is useful in research focused on T cell responses and MHC-TCR interactions, making it valuable for the study of immunological mechanisms and peptide-MHC complex dynamics. -
Peptide
OVA peptide is a class I (Kb)-restricted peptide epitope derived from ovalbumin, associated with the major histocompatibility complex (MHC) molecule H-2Kb in mice. This peptide plays a crucial role in immune response studies, particularly in allergy research, where it serves as a model antigen. Its ability to elicit specific T cell responses makes OVA peptide a valuable tool for understanding immune mechanisms and developing therapeutic strategies in allergy and immunology. -
Polypeptide
Gp100 (25-33), human is a polypeptide fragment comprising amino acids 25-33 of the human melanoma antigen. This 9-amino acid epitope is restricted by MHC class I H-2Db and elicits a specific T cell response due to its immunogenic properties. Gp100 (25-33), human is valuable for cancer research, particularly in studies focused on melanoma and T cell-mediated immune responses. -
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. -
TCIP 1 Ligand
BCL6-IN-13 is a potent inhibitor of the B-cell lymphoma 6 (BCL6) protein, demonstrating an IC50 value of 2 nM. This compound disrupts the interaction between BCL6 and its target proteins, leading to the activation of transcription factors involved in cellular growth and differentiation. BCL6-IN-13 is primarily utilized in research focused on B-cell malignancies, autoimmune disorders, and understanding the molecular mechanisms underlying oncology-related transcription regulation. -
BCL6 Degrader
BMS-986458 is a selective cereblon-based BCL6 degrader that exerts antitumor effects through the targeted degradation of the BCL6 protein. By binding to cereblon and interacting with the BTB domain of BCL6, it modulates key pathways such as cell cycle regulation, antiproliferative signals, and interferon responses, while also enhancing CD20 expression and distribution. BMS-986458 influences follicular helper T cell physiology and reduces circulating tumor DNA levels. Its combination with CD20xCD3 bispecific antibodies has been shown to improve T cell infiltration and expansion in tumors. This compound is applicable in research related to B-cell non-Hodgkin lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, and relapsed/refractory lymphoma. -
PROTAC BCL6 Degrader
PROTAC BCL6 Degrader-3 is a selective degrader targeting the BCL6 protein through the proteolysis-targeting chimera (PROTAC) approach. This compound mediates the ubiquitination and subsequent degradation of BCL6, facilitating the modulation of pathways associated with cancer and autoimmune diseases. It serves as a valuable tool for researchers exploring therapeutic strategies aimed at BCL6 inhibition and the underlying mechanisms of related diseases. -
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. -
EWSR1::FLI1 Binder
EB-TCIP is an EWSR1::FLI1 binder that operates by forming a ternary complex with the tagged fusion protein BCL6 and FKBP12F36V. This compound specifically recruits the EWSR1::FLI1 fusion to BCL6-associated DNA regions, leading to chromatin remodeling and the relocalization of transcriptional factors. As a result, EB-TCIP activates the expression of previously repressed BCL6 target genes. It serves as a valuable tool in the exploration of innovative epigenetic therapies for Ewing sarcoma. -
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. -
BCL-6 PROTAC Degrader
BCL6-760 is an orally active BCL-6 PROTAC degrader that selectively targets and degrades BCL-6 with an EC50 of 0.8 nM, without affecting other CRBN substrates. This compound exhibits notable efficacy in orthotopic xenograft mouse models of OCI-LY-1 tumors. BCL6-760 serves as a valuable tool for investigating diffuse large B-cell lymphoma (DLBCL) and for exploring mechanisms related to BCL-6 signaling pathways in cancer research. -
BCL6 PROTAC
BCL6 PROTAC 1 is a selective proteolysis targeting chimera (PROTAC) that targets B-cell lymphoma 6 (BCL6) for degradation. It exhibits potent inhibitory activity on BCL6 cell reporter assays, with an IC50 value of 8.8 µM. This reagent effectively induces degradation of BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines, making it a valuable tool for tumor-related research applications. -
BCL6 Ligand
BCL6 ligand-8 is a bifunctional linker designed to target the BCL6 protein for degradation via the PROTAC (Proteolysis Targeting Chimeras) mechanism. This compound plays a crucial role in the synthesis of PROTACs, including the effective BCL6-760, known for its anti-tumor properties. BCL6 ligand-8 is primarily utilized in cancer research to explore therapeutic strategies involving protein degradation pathways. -
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.
