Immunology & Inflammation

MRT199665 is a potent, ATP-competitive inhibitor targeting MARK, SIK, and AMPK pathways, exhibiting IC50 values of 2 nM for MARK1, 10 nM for AMPKα1, and 110 nM for SIK1. This compound induces apoptosis in MEF2C-activated human acute myeloid leukemia (AML) cells by effectively inhibiting the phosphorylation of the SIK substrate CRTC3 at S370. MRT199665 serves as a valuable tool for investigating the roles of MARK, SIK, and AMPK in cellular signaling and cancer biology.

Robinin is a flavonoid that acts as an inhibitor of Toll-like receptors 2 and 4 (TLR2/4), modulating the TGF-β, TLR4/NF-κB, and TLR2-PI3k-AKT signaling pathways. This compound demonstrates significant anti-inflammatory and anti-tumor properties. Additionally, Robinin has been shown to enhance the anti-inflammatory effects of Methotrexate in experimental arthritis models and may mitigate cardiac toxicity induced by Doxorubicin. These attributes make Robinin a valuable reagent for research applications in inflammation and cancer therapy.

Plantainoside D is a phenylethanoid glycoside that functions primarily as an inhibitor of IKK-β, with additional inhibitory effects on angiotensin-converting enzyme (ACE) and protein kinase C (PKC). It exhibits significant biological activities, including the reduction of glutamate release in the rat cerebral cortex, alleviating cell apoptosis through the inhibition of reactive oxygen species (ROS) and NF-κB activation. Additionally, Plantainoside D has been shown to improve outcomes in acute lung injury induced by sepsis via modulation of the Sirt3/NLRP3 signaling pathway. This compound is applicable in studies of neuroprotection, antioxidant activity, anti-inflammatory responses, and antihypertensive effects.

Nangibotide is a synthetic peptide that serves as a TREM-1 receptor inhibitor. By inhibiting NF-κB and NLRP3 inflammasome activation, Nangibotide effectively reduces the release of pro-inflammatory cytokines such as IL-1β and IL-8 and mitigates apoptosis. This reagent is valuable for research applications related to excessive inflammatory responses, including studies on myocardial ischemia-reperfusion injury, septic shock, acute lung injury, osteoarthritis, and acute liver failure. Additionally, Nangibotide offers protective effects on tissues, such as the liver and lung, during inflammatory conditions.

CPUY192018 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, exhibiting an IC50 of 0.63 µM. This compound demonstrates significant anti-inflammatory and antioxidant properties by activating the Nrf2-dependent pathway and inhibiting the NF-κB-related inflammatory response. CPUY192018 is ideal for research applications focused on inflammation-related diseases and the modulation of oxidative stress.

Lonicerin, also known as Veronicastroside, is a flavonoid recognized for its anti-inflammatory properties. It inhibits xanthine oxidase with an IC50 of 37.4 µg/mL and suppresses alginate secretion protein (AlgE). Lonicerin demonstrates a broad spectrum of biological activities, including antimicrobial effects against Pseudomonas aeruginosa and Candida albicans, as well as antioxidant and neuroprotective effects. Its diverse applications make it valuable in research focused on inflammation, infection, and oxidative stress.

Hederacoside C is a potent anti-inflammatory agent that targets the MAPK/NF-κB signaling pathway. It exerts its biological activity by inhibiting the activation of this pathway, resulting in a reduction of inflammation. In addition to its anti-inflammatory properties, Hederacoside C also demonstrates antibacterial activity, making it a valuable compound for research applications focused on inflammatory diseases and infections.

Muzastotug is a humanized immunoglobulin G1-kappa monoclonal antibody targeting CTLA-4 (Cytotoxic T-Lymphocyte-Associated Protein 4). It functions as both an immunostimulant and an antineoplastic agent. This antibody is designed to enhance the immune system's response against tumor cells by inhibiting CTLA-4, a protein that downregulates the immune response.

Vilastobart is a human IgG1 κ monoclonal antibody targeting CTLA-4. For accurate experimental control, it is recommended to use Human IgG1 kappa as an isotype control.

Sovipostobart is a human monoclonal antibody of the immunoglobulin G1-kappa class, specifically targeting CTLA-4 with a cleavable prodomain. It functions as both an immunostimulant and an antineoplastic agent. This biologic is designed to modulate the immune system by inhibiting CTLA-4, a protein that downregulates immune responses, thereby enhancing the body's antitumor activity. Sovipostobart is applicable in the study of immune checkpoint blockade therapies and is relevant for research focused on cancer immunotherapy.

Botensilimab (AGEN 1181) is a human monoclonal antibody that targets cytotoxic T-lymphocyte antigen 4 (CTLA-4), serving as both an innate and adaptive immune activator. This biologic is specifically designed for use in cancer research, where it facilitates the study of immune checkpoint blockade and its effects on tumor immunity.

Solasonine is a naturally occurring steroidal glycoalkaloid isolated from *Solanum melongena* (eggplant), known for its anti-infective, anticancer, and neurogenesis-promoting properties. It acts as a ferroptosis inducer by disrupting the glutathione redox system through inhibition of glutathione peroxidase 4 (GPX4). By promoting ferroptotic cell death in hepatocellular carcinoma (HCC) cells, Solasonine serves as a valuable compound for investigating ferroptosis mechanisms and developing novel anticancer strategies.

RMC-5127 is an orally active, brain-penetrant, mutant-selective tri-complex inhibitor targeting RASG12V. It non-covalently binds to cyclophilin A (CypA), forming a binary complex that engages active RASG12V to create a high-affinity tri-complex, thereby sterically blocking RAS-effector interactions. RMC-5127 inhibits RAS signaling in KRASG12V-mutant cancer cells, suppressing proliferation and inducing apoptosis. It holds promise for the study of RAS-mutant cancers, including non-small cell lung cancer.

Isofraxidin is a coumarin compound derived from *Acanthopanax senticosus* that exhibits anti-invasive and anti-inflammatory properties. It inhibits MMP-7 expression and suppresses cell invasion in human hepatoma cells by reducing ERK1/2 phosphorylation. Isofraxidin also downregulates the expression of iNOS and COX-2 and inhibits the formation of the TLR4/myeloid differentiation protein-2 (MD-2) complex.

JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist that effectively inhibits polymorphonuclear leukocyte mobilization with an EC₅₀ of 6.9 µM and reduces TNF levels with an EC₅₀ of 4.5 µM in mice. It is suitable for research in autoimmune and inflammatory diseases.

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.

MK-0159 is an orally active, potent, and selective inhibitor of CD38, with IC₅₀ values of 22 nM for human, 3 nM for mouse, and 70 nM for rat CD38. It exhibits good microsomal stability in both human and rodent liver microsomes. MK-0159 effectively increases NAD⁺ (nicotinamide adenine dinucleotide) levels and decreases ADPR (adenosine diphosphate ribose) concentrations in whole blood and heart tissue, making it a promising compound for research in metabolic, cardiovascular, and age-related diseases.

ADH-503 ((Z)-Leukadherin-1 choline) is an orally active, allosteric agonist of CD11b, an integrin subunit expressed on myeloid cells. By activating CD11b, ADH-503 promotes the repolarization of tumor-associated macrophages (TAMs) toward a pro-inflammatory phenotype, reduces the infiltration of immunosuppressive myeloid cells into tumors, and enhances dendritic cell responses. These immunomodulatory effects support its potential use in cancer immunotherapy.

JR14a is a potent thiophene-based antagonist of the human complement C3a receptor (C3aR). It exhibits high selectivity for C3aR over the C5a receptor and effectively suppresses C3aR-mediated inflammatory responses. JR14a is a valuable tool for studying the role of C3aR in immune regulation and inflammation-related diseases.

Phaseoloidin is a homogentisic acid glucoside isolated from *Nicotiana attenuata* trichomes. It plays a defensive role in the plant's resistance against lepidopteran herbivores by significantly reducing the growth of both specialist (*Manduca sexta*) and generalist (*Spodoptera littoralis*) larvae. In addition to its insect-deterrent properties, phaseoloidin also exhibits anti-complement activity, suggesting potential immunomodulatory applications.

Icotrokinra (JNJ-77242113) is an orally available and selective antagonist of the interleukin-23 (IL-23) receptor. It potently inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC₅₀ = 5.6 pM) and suppresses IL-23-induced interferon-γ (IFN-γ) production in natural killer (NK) cells (IC₅₀ = 18.4 pM). Icotrokinra also demonstrates anti-inflammatory activity in a rat TNBS-induced colitis model. It is a promising therapeutic candidate for the study and treatment of inflammatory conditions such as psoriasis, psoriatic arthritis, and inflammatory bowel disease (IBD).

Raleukin (AMG-719) is a recombinant, non-glycosylated human interleukin-1 receptor (IL-1R) antagonist. It functions by competitively inhibiting the binding of interleukin-1 (IL-1) to its receptor, thereby blocking IL-1–mediated pro-inflammatory signaling. As one of the first biological agents developed to inhibit IL-1 activity, Raleukin has potential applications in the treatment of inflammatory and autoimmune diseases.

Phenidone is an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX) pathways, exhibiting anti-inflammatory and immunomodulatory effects. It has been shown to ameliorate paralysis in rat models of experimental autoimmune encephalomyelitis (EAE), a model for multiple sclerosis. Phenidone also acts as a potent hypotensive agent in spontaneously hypertensive rats. Additionally, it has a long-standing application as a photographic developer due to its redox properties.

Glafenine is a non-selective, non-steroidal anti-inflammatory drug (NSAID) that inhibits both COX-1 and COX-2 enzymes. It exerts anti-inflammatory, anti-proliferative, and anti-migratory effects by suppressing the arachidonic acid metabolic pathway, thereby reducing prostaglandin production. Additionally, glafenine induces cell cycle arrest in vascular smooth muscle cells and endothelial cells and decreases the synthesis of the extracellular matrix protein tenascin. It is utilized in research related to inflammatory disorders, vascular restenosis, and cystic fibrosis.

L-NMMA acetate (NG-monomethyl-L-arginine acetate) is a non-selective nitric oxide synthase (NOS) inhibitor that targets all three NOS isoforms: neuronal (nNOS/NOS1), endothelial (eNOS/NOS3), and inducible (iNOS/NOS2). It exhibits Ki values of approximately 0.18 µM for rat nNOS, 0.4 µM for human eNOS, and 6 µM for mouse iNOS, making it a valuable tool for studying nitric oxide–mediated physiological and pathological processes.

CU-T12-9 is a specific and potent agonist of the Toll-like receptor 1/2 (TLR1/2) heterodimer, with an EC₅₀ of 52.9 nM in the HEK-Blue hTLR2 SEAP assay. It selectively activates TLR1/2 without affecting TLR2/6 and stimulates both innate and adaptive immune responses. CU-T12-9 signals through the NF-κB pathway, leading to elevated expression of downstream effectors such as TNF-α, IL-10, and iNOS, making it a valuable tool for immunological and inflammatory research.

LMT-28 is an orally active and the first synthetic interleukin-6 (IL-6) inhibitor that acts by directly binding to gp130, a key signal-transducing component of the IL-6 receptor complex. It selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130, exhibiting low toxicity. LMT-28 is a promising compound for research into IL-6-mediated inflammatory and autoimmune diseases.

Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active, non-selective cyclooxygenase (COX) inhibitor. It exhibits analgesic, anti-inflammatory, and anti-cancer effects. As the active enantiomer of ketoprofen, Dexketoprofen trometamol is commonly used for the management of pain and inflammation, and it is also under investigation for its potential anticancer properties.