Immunology & Inflammation

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.

EG01377 dihydrochloride is a potent, bioavailable, and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM and IC₅₀ values of 609 nM for both NRP1-a1 and NRP1-b1 domains. It exhibits antiangiogenic, antimigratory, and antitumor activities.

Perforin-IN-2 (Compound 1) is a perforin inhibitor that blocks perforin-mediated cell lysis. It has potential to reduce graft rejection in the context of allogeneic bone marrow or stem cell transplantation.

Lipoteichoic acid is an orally active compound with anti-inflammatory and antitumor properties. It is a key immune molecule found in Gram-positive bacteria that activates the complement system by upregulating C3 and inhibiting CD55. Lipoteichoic acid modulates macrophage autophagy via the PI3K/Akt/mTOR pathway, induces lung injury in mouse models, and inhibits melanin production.

Vemircopan (ALXN2050) is an orally active inhibitor of complement factor D (FD). It is being investigated for the treatment of complement-mediated diseases, including myasthenia gravis, lupus nephritis, IgA nephropathy, and paroxysmal nocturnal hemoglobinuria (PNH).

W-54011 is a potent, orally active, non-peptide antagonist of the C5a receptor. It inhibits the binding of \[¹²⁵I]-labeled C5a to human neutrophils with a Kᵢ of 2.2 nM. W-54011 also suppresses C5a-induced intracellular Ca²⁺ mobilization, chemotaxis, and reactive oxygen species (ROS) generation in human neutrophils, with IC₅₀ values of 3.1 nM, 2.7 nM, and 1.6 nM, respectively.

C3a Receptor Agonist 1 (a benzeneacetamide derivative) is a potent agonist of the C3a receptor. It holds potential for research in acute inflammation and complement system–mediated responses.

Cemdisiran is an N-acetylgalactosamine (GalNAc)-conjugated small interfering RNA (siRNA) designed to suppress hepatic production of complement component 5 (C5). It is used in research focused on complement-mediated diseases.

BM213 is a potent and selective agonist of C5aR1 that demonstrates antitumor activity in a mouse model of mammary carcinoma.

NDT 9513727 is a potent, selective, orally active, and competitive inverse agonist of the human C5a receptor (C5aR), with an IC₅₀ of 11.6 nM. It is suitable for research in human inflammatory diseases.

Pelecopan (BCX9930) is a potent, selective, and orally active inhibitor of complement factor D, with an IC₅₀ value of 14.3 nM. It targets factor D to prevent both intravascular and extravascular hemolysis in paroxysmal nocturnal hemoglobinuria (PNH) and is also applicable to other diseases mediated by the alternative complement pathway.

BR103 is a C3a receptor (C3aR)-specific small molecule ligand. It is useful for measuring ligand affinity to G protein-coupled receptors (GPCRs) through saturation and competitive binding assays.

LyP-1 is a cyclic 9-amino-acid tumor-homing peptide that selectively binds to p32 receptors, which are overexpressed on various tumor-associated cells.

Zoracopan is a selective inhibitor of complement factor D (CFD). Upon systemic administration (oral or intravenous), it preferentially accumulates in ocular tissues and is released in a sustained manner, primarily targeting the choroid–retinal pigment epithelium (C-RPE) and/or iridociliary body (I-CB).

CP-447697 is a lipophilic C5a receptor antagonist with an IC₅₀ value of 31 nM. It is suitable for research related to inflammation and complement system modulation.

Campneoside II is a natural compound isolated from the wood of *Paulownia tomentosa* var. *tomentosa*. It exhibits potent anti-complement activity.

PIC1 PA is a 15-amino-acid peptide and a potent analog of PIC1 that inhibits classical pathway–mediated complement activation. It functions by disrupting the interaction between C1s-C1r-C1r-C1s/MASPs and the collagen-like region (CLR) of C1q or MBL. PIC1 PA specifically binds to the CLR of C1q, with a mean equilibrium dissociation constant (K\_D) of 33.3 nM for purified C1q.

tLyP-1 peptide is a neuropilin-1 (NRP-1) targeting peptide with an IC₅₀ of 4 μM and the amino acid sequence CGNKRTR. It specifically binds to NRP-1, enabling selective targeting of tumor cells.

L-156602 is a C5a receptor antagonist that inhibits inflammation and blocks the migration of monocytes and neutrophils to sites of infiltration in mouse inflammatory models. It also suppresses the efferent phase of delayed-type hypersensitivity (DTH).

Tarvicopan is an inhibitor for complement factor D.

Lanoracopan is a potent inhibitor of complement factor B, with an IC₅₀ of 1.2 μM. It is suitable for research in inflammation- and immunity-related diseases.

CP-289,503 is an inhibitor of the complement C5a receptor, with an IC₅₀ of 1 μM. The C5a receptor mediates pro-inflammatory signaling by binding to C5a, a complement activation product that stimulates leukocyte and phagocyte activation, upregulates integrins, and induces degranulation of inflammatory cells, contributing to endothelial damage. By blocking C5a signaling, CP-289,503 may be useful in the treatment of various inflammatory diseases.

DB0614 is a PROTAC molecule utilizing a cereblon ligand, designed as a selective and potent degrader of NEK9 and other kinases. It induces the degradation of multiple kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1–3, MAP4K5, MAPK14, MAPK7–9, MAPKAPK2/3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1/3, SIK2/3, STK35, TNK2, and ULK1. DB0614 is suitable for research involving diseases or disorders driven by aberrant kinase activity.

MY-1B is a covalent inhibitor of the RNA methyltransferase NSUN2 (IC50: 1.3 μM), stereoselectively targeting active-site cysteine residues (C271). It also covalently binds to PSME1, disrupting the proteasome regulatory complex and downregulating specific MHC-I subtype presentation.