Immunology & Inflammation

Glafenine hydrochloride is a non-selective non-steroidal anti-inflammatory agent and a dual inhibitor of COX-1 and COX-2 enzymes. It demonstrates anti-inflammatory, anti-proliferative, and anti-migratory effects by disrupting the arachidonic acid metabolic pathway and decreasing prostaglandin synthesis. This compound induces cell cycle arrest in vascular smooth muscle and endothelial cells, while also lowering Tenascin levels in the extracellular matrix. Glafenine hydrochloride is applicable in the study of inflammatory diseases, vascular restenosis, and cystic fibrosis.

Proanthocyanidins are a class of polyphenolic compounds characterized by their electrophilic flavanyl units, primarily recognized for their anti-inflammatory properties. They exhibit strong antioxidant activity and have been shown to possess anticancer effects, as well as cardioprotective, antibacterial, and antifungal activities. Research applications include their potential use in treating conditions such as chronic venous insufficiency, capillary fragility, sunburn, and retinopathy.

Lenalidomide hemihydrate functions as a molecular glue through its activity as an immunomodulator. This compound selectively binds to the ubiquitin E3 ligase cereblon (CRBN), leading to the ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 via the CRBN-CRL4 complex. Lenalidomide hemihydrate is effective in inhibiting the proliferation of mature B-cell lymphomas, including multiple myeloma, and promotes the release of IL-2 from T cells, making it a valuable tool in cancer research.

Seselin is an anti-inflammatory agent that exerts its effects through multiple biological pathways. It has demonstrated potential in anticancer, antinociceptive, and antifungal activities. Seselin is suitable for research applications focused on inflammation and pain management. Its oral bioavailability enhances its utility in vivo studies.

Nepetoidin B is an anti-inflammatory agent that exerts its effects by modulating the NF-κB and Nrf2/HO-1 signaling pathways. In addition to its anti-inflammatory properties, Nepetoidin B also demonstrates antifungal and antibacterial activities. This natural compound, derived from Salvia plebeia R. Br., is suitable for research applications focused on inflammation and infectious diseases.

Myristinin A is a flavan compound that exhibits anti-inflammatory properties by selectively inhibiting COX-2 activity, with an IC50 value of 16.9 μg/mL. It reduces the production of prostaglandin E2 (PGE2) and inhibits phospholipase A2 (PLA2), effectively blocking the release of inflammatory mediators. Additionally, Myristinin A demonstrates antifungal activity against Candida albicans, with an IC50 of 8.8 μg/mL. This compound is valuable for research into inflammation and infection, particularly in conditions such as rheumatoid arthritis.

Corydalmine, a CXCR inhibitor, demonstrates significant antifungal activity by inhibiting spore germination in various plant pathogenic and saprophytic fungi. Additionally, it serves as an oral analgesic agent, exhibiting potent analgesic effects. Corydalmine has been shown to alleviate Vincristine-induced neuropathic pain in murine models through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, making it a valuable tool for pain research and therapeutic applications.

CYP51/PD-L1-IN-3 is a dual inhibitor targeting CYP51 and PD-L1, exhibiting potent antifungal activity with IC50 values of 0.205 μM and 0.039 μM, respectively. This compound induces early apoptosis in fungal cells by reducing levels of intracellular IL-2, NLRP3, and NF-κBp65 proteins. Additionally, CYP51/PD-L1-IN-3 causes mitochondrial damage and reactive oxygen species (ROS) accumulation, ultimately resulting in fungal lysis and cell death. This compound serves as a valuable tool for research in fungal infections and immune modulation.

CYP51/PD-L1-IN-2 is a quinazoline compound that functions as a dual inhibitor of CYP51 and PD-L1, exhibiting IC50 values of 0.263 μM and 0.017 μM, respectively. It displays notable antifungal activity by triggering early apoptosis in fungal cells, leading to significant reductions in intracellular IL-2, NLRP3, and NF-κBp65 protein levels. Additionally, CYP51/PD-L1-IN-2 induces mitochondrial damage and reactive oxygen species (ROS) accumulation, culminating in fungal lysis and subsequent cell death. This compound is valuable for research exploring antifungal mechanisms and cancer immunotherapy.

CYP51/PD-L1-IN-1 is a dual inhibitor targeting both CYP51 and PD-L1, exhibiting an IC50 of 0.884 μM for CYP51 and 0.083 μM for PD-L1. This quinazoline compound demonstrates notable antifungal activity by inducing early apoptosis in fungal cells while significantly reducing intracellular levels of IL-2, NLRP3, and NF-κBp65. Additionally, CYP51/PD-L1-IN-1 contributes to mitochondrial damage and reactive oxygen species (ROS) accumulation, ultimately leading to fungal lysis and cell death. This compound is valuable for research focused on antifungal therapies and immune modulation.

Corydalmine hydrochloride is a potent CXCR inhibitor that demonstrates significant biological activity by inhibiting spore germination in certain plant pathogenic and saprophytic fungi. Additionally, it exhibits notable analgesic properties, effectively alleviating Vincristine-induced neuropathic pain in murine models. This effect is mediated through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, highlighting its potential applications in pain management research and fungal inhibition studies.

Nyasol is a bioactive compound known for its anti-inflammatory and antimicrobial properties. It demonstrates significant antifungal, antibacterial, and antileishmanial activities, alongside hyaluronidase inhibition. Nyasol effectively inhibits the binding of leukotriene B4 (LTB4) to human neutrophils and suppresses neuroinflammatory responses by inhibiting I-κB degradation in lipopolysaccharide-stimulated BV-2 microglial cells. This compound is valuable in research focused on inflammatory diseases and microbial infections.

Porustobart is a monoclonal antibody specifically targeting CTLA-4 (Cytotoxic T-Lymphocyte-Associated Protein 4). This antibody is designed for use in research studies to investigate the modulation of immune checkpoints, which are crucial for understanding immune system behavior in cancer and other diseases. Porustobart can be utilized in various experimental settings, including flow cytometry, Western blotting, and immunoprecipitation, making it a valuable tool for researchers focusing on immunology and oncology.

Anti-CTLA-4/CD152 Antibody (BN13) is a chimeric mouse IgG2a, κ antibody designed to target human CTLA-4/CD152. For isotype control, it is recommended to use Mouse IgG2a kappa, Isotype Control, ensuring specificity and consistency in antibody performance.

Bavunalimab is a bispecific monoclonal antibody targeting CTLA-4 and LAG-3, designed for the dual inhibition of these immune checkpoint inhibitors. This humanized antibody promotes T-cell activation, demonstrated in NSG mouse models, making it a valuable tool for investigating immune responses in oncology research. Bavunalimab is specifically developed for studies focusing on the modulation of immune checkpoints in cancer therapy.

Zalifrelimab (AGEN1884) is a fully human IgG1 monoclonal antibody designed to specifically target and inhibit CTLA-4 (Cytotoxic T-Lymphocyte-Associated Protein 4). By antagonizing the inhibitory checkpoints mediated by CTLA-4 signaling, Zalifrelimab enhances immune cell activation, potentially amplifying antitumor immune responses. This antibody is utilized in research focused on immunotherapy and the modulation of immune checkpoints in oncology.

Nurulimab (BCD-145) is a human monoclonal antibody that targets cytotoxic T lymphocyte antigen-4 (CTLA-4). This antibody is specifically designed for use in melanoma research, where it can help investigate the role of CTLA-4 in tumor immunity and potential therapeutic interventions.

Tremelimumab (Ticilimumab) is a fully human monoclonal antibody specific for cytotoxic T-lymphocyte antigen-4 (CTLA-4) and can be used for metastatic melanoma research.

Encelimab is a monoclonal antibody targeting LAG-3 (Lymphocyte-activation gene 3). By inhibiting the interaction between LAG-3 and MHC class II molecules, Encelimab promotes T-cell activation and enhances immune responses. Studies have demonstrated that Encelimab, both as a monotherapy and in conjunction with an anti-PD-1 antibody, effectively reduces tumor volume in a lymphoma mouse model using A20 cell xenografts. This antibody is pivotal for research focused on immunotherapy and cancer immunology, particularly in understanding and manipulating T-cell responses in oncological models.

The Anti-CTLA-4/CD152 Antibody is a humanized monoclonal antibody produced in Chinese Hamster Ovary (CHO) cells, specifically targeting CTLA-4 (CD152). This antibody comprises a human IgG4SP heavy chain and a human kappa light chain, with an approximate molecular weight of 145 kDa. For experimental controls, the recommended isotype control is Human IgG1 kappa. This antibody is essential for research focusing on immune checkpoint regulation and cancer immunotherapy.

Firastotug is an IgG1κ monoclonal antibody specifically designed to target CTLA-4, a critical immune checkpoint protein associated with cytotoxic T lymphocytes. CTLA-4 plays a pivotal role in regulating immune responses, making it a significant target in the study of autoimmunity and oncology. This antibody is instrumental for researchers focusing on the modulation of immune checkpoints to understand disease mechanisms and develop therapeutic strategies.

Cadonilimab (AK104) is a humanized tetravalent IgG1 bispecific antibody designed to simultaneously target PD-1 and CTLA-4. By inhibiting these checkpoint pathways, Cadonilimab effectively alleviates immunosuppression and reverses T cell exhaustion specific to tumor environments. This antibody notably reduces Fc-mediated effector functions, including antibody-dependent cell-mediated cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), and complement-dependent cytotoxicity (CDC). Cadonilimab is applicable in research focused on metastatic cervical cancer and other malignancies, including gastric cancer, gastroesophageal junction (GEJ) adenocarcinoma, and non-small cell lung cancer (NSCLC), providing a valuable tool for investigations into immune checkpoint blockade and cancer immunotherapy.

Favezelimab (MK-4280) is a humanized monoclonal antibody targeting LAG-3, designed to inhibit the binding of LAG-3 to MHC class II molecules. This interaction blockade enhances T-cell function and may potentiate an anti-tumor immune response. Favezelimab is primarily investigated for its therapeutic potential in colorectal cancer research, particularly in combination with the PD-L1 inhibitor Pembrolizumab, to synergistically enhance immune-mediated tumor suppression.

Evalstotug is a human IgG1 κ monoclonal antibody targeting CTLA-4 (Cytotoxic T-Lymphocyte-Associated protein 4). For accurate experimental control, it is recommended to use Human IgG1 kappa isotype control.

Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting antibody (DART) designed to simultaneously inhibit the activity of PD-1 and CTLA-4 immune checkpoints. By blocking these pathways, Lorigerlimab enhances T-cell mediated immune responses, which are critical in the control and elimination of tumors. This antibody is particularly relevant for studies focused on metastatic castration-resistant prostate cancer (mCRPC), providing a valuable tool for research in immune checkpoint blockade therapies and their role in cancer immunology.

Fianlimab (REGN3767) is a human monoclonal antibody designed to specifically bind to the lymphocyte-activation gene 3 (LAG-3) immune checkpoint receptor expressed on T cells. This interaction inhibits the LAG-3 pathway, thereby enhancing T cell function and exhibiting potent anti-tumor activity. Fianlimab is utilized in oncological research to investigate immune checkpoint blockade as a strategy for cancer immunotherapy.

Tuparstobart (Incagn-02385) is an IgG1κ monoclonal antibody designed to specifically target LAG-3, an immune checkpoint receptor. LAG-3 is predominantly expressed on activated T cells, NK cells, B cells, and plasmacytoid dendritic cells. This antibody is engineered to bind to LAG-3, thereby modulating immune responses, which may be critical in the research of immune regulation and potential therapeutic applications in immune-related disorders.

Relatlimab (BMS-986016) is a human monoclonal antibody targeting LAG-3, developed through the immunization of transgenic mice engineered to express human immunoglobulin miniloci, using recombinant LAG-3 protein. This antibody effectively inhibits the interaction between LAG-3 and MHC II with an IC50 of 0.67 nM, and between LAG-3 and FGL1 with an IC50 of 0.019 nM. It is primarily utilized in cancer research, providing a valuable tool for investigating the role of LAG-3 in tumor immune evasion and potential therapeutic interventions.

Erfonrilimab (KN-046) is a bifunctional monoclonal antibody designed to simultaneously inhibit both PD-L1 and CTLA-4, two critical immune checkpoint proteins. This dual inhibition mechanism enhances the immune system's ability to recognize and destroy cancer cells, making it a promising therapeutic agent in oncology research. Erfonrilimab is specifically engineered for use in investigating the efficacy of combined checkpoint blockade in various cancer models.

Miptenalimab (BI-754111) is a monoclonal antibody targeting human LAG-3 with a dissociation constant (K_D) of 88.6 nM. This antibody effectively inhibits the interaction between LAG-3 and its physiological ligand MHC class II, highlighting its potential utility in modulating immune responses in oncological and immunological research.

Ipilimumab is a fully human monoclonal antibody of the IgG1κ isotype designed to inhibit the cytotoxic T lymphocyte antigen 4 (CTLA-4) receptor on T cells. This antibody is utilized in research focused on unresectable or metastatic melanoma (MM), serving as a critical tool in investigating the modulation of immune checkpoints in cancer therapy.

Negalstobart is a human IgG4 κ monoclonal antibody targeting LAG-3. For control experiments, it is recommended to use Human IgG4 (S228P) kappa as an isotype control.

Resolvin D3 (RvD3) is a bioactive mediator derived from docosahexaenoic acid (DHA) with potent anti-inflammatory properties. This compound plays a crucial role in resolving inflammation, making it particularly relevant for research into inflammatory conditions such as arthritis. By modulating immune responses, Resolvin D3 facilitates the resolution of inflammation, providing insights into therapeutic strategies for inflammatory diseases.

Carvedilol-d3 is a deuterium-labeled analogue of Carvedilol, functioning primarily as a non-selective β/α-1 adrenergic receptor blocker. It exhibits significant biological activity by inhibiting lipid peroxidation in a dose-dependent manner with an IC50 value of 5 μM. This compound serves as a versatile antihypertensive agent and has potential applications in the treatment of angina and congestive heart failure. Furthermore, Carvedilol-d3 promotes autophagy and is known to inhibit the NLRP3 inflammasome, making it valuable for research involving inflammatory processes.

Carvedilol-d5 is a deuterium-labeled analogue of Carvedilol, a non-selective β/α-1 adrenergic receptor blocker. It exhibits lipid peroxidation inhibition with an IC50 of 5 μM and serves as a versatile antihypertensive agent, showing potential in the treatment of angina and congestive heart failure. Additionally, Carvedilol functions as an autophagy inducer and inhibits the NLRP3 inflammasome, making it relevant for research in inflammatory pathways and cardiovascular health.

Indomethacin farnesil is a prodrug of indomethacin, primarily targeting cyclooxygenase (COX) enzymes. This potent, blood-brain barrier-permeable inhibitor exhibits nonselective activity against COX-1 and COX-2, with IC50 values of 18 nM and 26 nM, respectively. Indomethacin farnesil has been shown to disrupt autophagic flux by impairing lysosomal function, making it useful for investigating inflammatory pathways and autophagy-related processes in research applications.

SBP-5147 is a potent inhibitor of ULK1 and ULK2, exhibiting an IC50 of 2 nM for ULK1 and 53 nM for ULK2. This compound effectively inhibits the phosphorylation of Beclin-1 and Vps34, reduces autophagic flux, and downregulates the expression of key autophagy-related proteins ATG13 and ATG101. Additionally, SBP-5147 enhances MHC-I expression, induces caspase-dependent apoptosis, and decreases the viability of non-small cell lung cancer cells. Its mechanism of action makes SBP-5147 a valuable tool for research in non-small cell lung cancer and autophagy modulation.

Z-Val-Val-Nle-diazomethylketone is a selective inhibitor of cathepsin S (CATS). This compound effectively reduces the IFNg-induced upregulation of MHCII molecules, specifically HLA-DR and Ii-p33/35, while promoting an increase in the Ii-p10 protein level. It is valuable for research into dermatological conditions such as psoriasis, atopic dermatitis, and actinic keratosis.

Fmoc-Leucine, an anti-inflammatory agent, functions primarily as a selective ligand for PPARγ, with a binding affinity (Ki) of 15 μM. It promotes both extracellular Ca2+ influx and intracellular Ca2+ release while exhibiting insulin-sensitizing effects with minimal fatogenic activity. This compound demonstrates unique self-assembly characteristics, forming transient gels, stable gels, or crystals/2D sheets under varying conditions. Fmoc-Leucine is valuable for research related to diabetes, colitis, and bladder cancer.

Hexadecanamide is a fatty acid amide that serves as an anti-inflammatory agent, exhibiting protective effects against Staphylococcus aureus and SARA-induced mastitis. It functions by suppressing S. aureus-mediated NF-κB activation and enhancing blood-milk barrier integrity. Additionally, Hexadecanamide activates PPARα and has been shown to improve sperm motility in vitro. This compound is relevant for research applications involving mastitis and asthenozoospermia.

Norathyriol is a natural metabolite derived from Mangifera, exhibiting significant anti-inflammatory and anticancer properties. It functions as a noncompetitive inhibitor of α-glucosidase with an IC50 value of 3.12 μM. Additionally, Norathyriol inhibits the peroxisome proliferator-activated receptors (PPARs) α, β, and γ, with IC50s of 92.8 μM, 102.4 μM, and 153.5 μM, respectively. This compound demonstrates a range of biological activities, including antioxidant, antimicrobial, and antibacterial effects, making it valuable for diverse research applications in inflammation and cancer therapeutics.

1-O-Hexadecylglycerol serves as an anti-inflammatory agent by upregulating PPAR-γ expression and inhibiting prostaglandin E2 (PGE2) synthesis. This compound demonstrates significant biological activity in reducing inflammation and is suitable for various research applications focused on inflammatory processes. Its efficacy is noted in oral administration, facilitating its potential use in preclinical studies and therapeutic exploration.

Adelmidrol is an anti-inflammatory agent that primarily targets peroxisome proliferator-activated receptor gamma (PPARγ). This compound mediates significant reductions in NF-κB translocation and COX-2 expression, contributing to its anti-inflammatory effects. Adelmidrol is utilized in research focused on inflammation pathways and therapeutic potential in various inflammatory conditions.

YS121 is a dual inhibitor targeting microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LOX), with IC50 values of 3.4 μM and 6.5 μM, respectively. It demonstrates specific, reversible binding to mPGES-1, indicated by a KD of 10-14 μM. YS121 reduces PGE2 production in IL-1β-stimulated A549 cells with an EC50 of 12 μM and activates PPAR-α and PPAR-γ, with EC50 values of 1 μM and 3.6 μM, respectively. Additionally, YS121 exhibits significant anti-inflammatory effects in human whole blood and in vivo, making it a valuable tool for pleurisy research.

3-Aminoisobutyric acid is an anti-inflammatory agent that exhibits both anti-inflammatory and antioxidant properties. It enhances the expression of genes associated with brown adipocytes in white adipose tissue and promotes fatty acid β-oxidation in hepatocytes. Additionally, 3-Aminoisobutyric acid mitigates insulin resistance and inflammation triggered by palmitate or a high-fat diet through an AMPK-PPARδ-dependent pathway in murine models. This compound also serves as a catabolic metabolite of thymine and valine within skeletal muscle, making it relevant for metabolic research.

Romazarit, a PPARα agonist, serves as an effective anti-inflammatory agent with demonstrated antirheumatic properties. In studies, Romazarit has been shown to inhibit the development of hindpaw inflammation at a dosage of 30 mg/kg in an adjuvant arthritis model. This compound is of interest for research applications focusing on inflammatory diseases and therapeutic interventions in arthritis.

(3R,5R)-3,5-Dihydroxy-1,7-bis(3,4-dihydroxyphenyl)heptane 3-O-β-D-glucopyranoside functions as an anti-inflammatory agent. This diarylheptanol glycoside, derived from Tacca plantaginea, effectively inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 9.4 μM. Additionally, it activates PPAR transcriptional activity (EC50 = 9.9 μM) and exhibits a specific activating effect on PPAR β(δ) with an EC50 of 23.1 μM. Non-toxic to cells at tested concentrations, this compound is suitable for research on inflammatory conditions.

Zaltoprofen sulfoxide is a selective COX-2 inhibitor with an IC50 of 45.38 nM, as well as a PPAR-γ activator. This compound effectively inhibits NF-κB and MAPK inflammatory signaling pathways, making it a valuable tool in the study of inflammation and acute lung injury models. It is particularly relevant for research focused on LPS-induced acute lung injury.

Dihydrolipoic Acid (DHLA) is a potent antioxidant primarily targeting reactive oxygen species. It demonstrates significant anti-inflammatory effects across various disease models. Research indicates that DHLA can modulate the ERK/Nrf2/HO-1/ROS/NLRP3 signaling pathway, effectively mitigating sickness behavior in LPS-induced rat models. This compound is valuable for studies related to depression and oxidative stress-related disorders.

Nrf2-IN-3 is a small-molecule inhibitor targeting Nrf2 by enhancing the production of reactive oxygen species (ROS). It specifically binds to KEAP1 mutants, restoring their ability to inhibit Nrf2 and facilitating proteasome-dependent degradation of Nrf2 in cells. This compound has shown potential in sensitizing KEAP1-mutated tumor cells to chemotherapeutic agents such as Cisplatin and Gefitinib, making it a valuable tool for research in cancer therapeutics and Nrf2-related signaling pathways.