IL Receptor

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  1. Suplatast Tosilate is a novel capsular anti-asthmatic agent that suppresses both IgE production, IL-4 and IL-5 synthesis with IC50 above 100 μM.
  2. IL-17 inhibitor

    Y320 is an orally active immunomodulator, and inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 of 20 to 60 nM.
  3. immunopotentiator

    Inosine pranobex is a potent, broad-spectrum antiviral compound for HIV infection. Inosine pranobex is an immunopotentiator.
  4. IL-1 inhibitor

    IX 207-887 is a novel antiarthritic agent which inhibits the release of interleukin-1 (IL-1).
  5. gp130 inhibitor

    SC-144 is an orally active small-molecule gp130 inhibitor.
  6. IL-12/IL-23 inhibitor

    Apilimod is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-r/LPS?Cstimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.
  7. T cell activator

    beta-Interleukin I (163-171), human, a peptide. Interleukins are a group of cytokines (secreted proteins/signaling molecules) that were first seen to be expressed by white blood cells (leukocytes).
  8. anti-cancer agent

    Ginsenoside Rc, isolated from Panax ginseng, may exert various activities including anti-cancer, anti-inflammatory, antiobesity, and anti-diabetic effects.
  9. interleukin-5 receptor antagonist

    YM-90709 is an interleukin-5 receptor antagonist. YM-90709 inhibits the binding of IL-5 to its receptor on peripheral human eosinophils and butyric acid-treated eosinophilic HL-60 clone 15 cells, with IC50 values of 1.0 and 0.57 microM, respectively.
  10. IL-12/23 inhibitor

    APY0201 is a potent and selective IL-12/23 inhibitor.
  11. IL-1 inhibitor

    AS101, a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.
  12. IL-1 receptor antagonist

    AF 12198 is a potent and selective antagonist for the human type I interleukin-1 (IL-1) receptor.
  13. Balsalazide sodium hydrate could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
  14. anti-inflammatory agent

    Balsalazide is an anti-inflammatory agent for treatment of Inflammatory Bowel Disease. Balsalazide could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
  15. Neuroinflammation inhibitor

    GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM).
  16. gp130 modulator

    RCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.
  17. IL-2 synthesis inhibitor

    NFAT Transcription Factor Regulator-1 is an IL-2 synthesis inhibitor with an IC50 of 182 nM.
  18. IL receptor agonist

    NO-prednisolone is a nitric oxide (NO)-releasing derivative of Prednisolone. NO-prednisolone potently stimulates IL-10 production in vivo.
  19. interleukin inhibitor

    RP-54745 is an inhibitor of macrophage stimulation and interleukin-1 production, and a potential antirheumatic compound.
  20. Smurf1 inhibitor

    Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation.
  21. IL-2 inducer

    Nosantine racemate is the racemate of Nosantine. Nosantine is an inducer of IL-2 or enhancer of IL-2 induction by phytohemagglutinin (PHA).
  22. IL-15 inhibitor

    IL-15-IN-1 is a potent and selective Interleukin 15 (IL-15) inhibitor, inhibiting the proliferation of IL-15-dependent cells with an IC50 of 0.8 μM.
  23. Dexanabinol exhibits not only the antioxidant and neuroprotective activities in brain but also anti-inflammatory activity by inhibiting NF-κB and decreasing cytokines such as TNFα and interleukin-6, which could ensure the integrity of BBB and reduce cell apoptosis and death.
  24. Tyrphostin A1(AG9) inhibits CD40L-stimulated IL-12 production in macrophage cultures and antigen-induced generation of Th1 cells.
  25. Gamma-glutamylcysteine (TFA) ((γ-glutamylcysteine (TFA)), an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx).
  26. IL-12/IL-23 inhibitor

    Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively.
  27. IL-2 inhibitor

    SU5201 is an inhibitor of interleukin-2 (IL-2) production.
  28. IL-23 receptor antagonist

    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).
  29. IL-1R antagonist

    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.
  30. IL-6 inhibitor

    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.
  31. 6-Demethoxytangeretin is a flavonoid compound isolated from *Citrus reticulata* with demonstrated anti-inflammatory and anti-allergic properties. It inhibits IL-6 production and the expression of related genes in human mast cells by modulating the ALK and MAPK signaling pathways. Additionally, 6-Demethoxytangeretin enhances CRE-mediated transcription in hippocampal neurons, indicating potential neuroregulatory effects.
  32. PPAR agonist

    Lobeglitazone is a novel thiazolidinedione-class compound and an orally active dual agonist of peroxisome proliferator-activated receptors (PPARs), with EC₅₀ values of 137.4 nM for PPARγ and 546.3 nM for PPARα. In addition to its metabolic effects, Lobeglitazone functions as an inhibitor of multiple pro-inflammatory and pro-fibrotic signaling pathways, including ERK, JNK, Smad, and NF-κB. Lobeglitazone exhibits a broad range of pharmacological activities, including anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic effects. These properties make it a promising candidate for therapeutic research in metabolic syndrome, type 2 diabetes, cardiovascular disease, and fibrosis-related conditions.
  33. Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue that exhibits potent anti-inflammatory activity. It exerts its effects by blocking mitogen-activated protein kinase (MAPK) signaling and inhibiting the nuclear translocation of the NF-κB subunit p65, thereby suppressing key inflammatory pathways. Additionally, compound 5a27 reduces neutrophil infiltration and the production of pro-inflammatory cytokines. In vivo, it significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI), highlighting its potential as a therapeutic candidate for inflammatory and respiratory disorders.
  34. Lysophosphatidylcholines (LPCs) are orally active lysolipids and key components of oxidized low-density lipoprotein (oxLDL). They are bioactive molecules known to induce cellular injury, promote the production of pro-inflammatory cytokines such as interleukin-1β (IL-1β), and trigger apoptosis. LPCs play a significant role in the pathophysiology of various inflammatory conditions and have been implicated in the progression of sepsis by amplifying inflammatory responses. Due to these properties, LPCs are actively studied in the context of inflammation, cardiovascular disease, and sepsis-related research.
  35. Rab27a-JFC1 Inhibitor

    Nexinhib20 is a selective inhibitor of the Rab27a-JFC1 interaction (IC50: 2.6 μM) and Rac-1-GTP signaling. This compound effectively inhibits neutrophil exocytosis, adhesion, and β2 integrin activation, demonstrating significant anti-inflammatory properties. Nexinhib20 is suitable for research applications focused on systemic inflammation and myocardial ischemia-reperfusion injury.
  36. ATP

    Endogenous Metabolite

    ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation. ATP can activate the NLRP3 inflammasome and induce IL-1β and chemokines secretion. ATP has anti-bacterial infection effects and can protect mice against bacterial infection in mice.
  37. PDE Inhibitor

    Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD).
  38. AMPK Agonist

    10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis.
  39. TNF Receptor Inhibitor

    Muscone, a TNF receptor inhibitor, is derived from the traditional Chinese medicine musk. It effectively inhibits NF-κB signaling and NLRP3 inflammasome activation, resulting in a significant reduction of inflammatory cytokines such as IL-1β, TNF-α, and IL-6. This compound is valuable in research focused on inflammation, cardiac function restoration, and improving survival rates in various pathological conditions.
  40. Anti-Inflammatory/Antibacterial Agent

    (20R)-Protopanaxadiol acts as an anti-inflammatory and antibacterial agent, derived from ginsenosides. It effectively exhibits anti-inflammatory properties while maintaining a lack of significant cytotoxicity against tumor cell lines. Additionally, (20R)-Protopanaxadiol has been shown to inhibit the uptake of 2-deoxy-D-glucose (2-DG), making it relevant for research applications focusing on metabolic pathways and the modulation of inflammatory processes.
  41. IL-1 Inhibitor

    Diacerein is a potent IL-1 inhibitor that functions by reducing the production of IL-1 converting enzyme, thereby inhibiting the activation of IL-1β and its downstream signaling pathways. This compound exhibits significant anti-inflammatory and anti-rheumatic properties, making it useful for various research applications, including studies on osteoarthritis and the management of bronchospasm and airway inflammation in asthmatic models. Diacerein is recognized as a slow-acting drug for symptomatic relief of osteoarthritis, facilitating insights into long-term therapeutic strategies.
  42. Histamine H1 Receptor Antagonist

    Epinastine is a selective histamine H1 receptor antagonist, known for its effectiveness as a mast cell stabilizer. It exhibits high affinity for neuronal octopamine receptors in various insects, demonstrating potential roles in modulating immune responses. Epinastine also inhibits pro-inflammatory cytokines such as TARC, IL-8, and IL-4, making it valuable for research into allergic diseases and anti-cancer immunity mechanisms. Its ability to reduce scratching behavior and vascular permeability further underscores its relevance in studying allergic and inflammatory conditions.
  43. IL-1β Converting Enzyme Inhibitor

    SDZ 224-015 is a potent inhibitor of the interleukin-1 beta (IL-1β) converting enzyme and caspase-1, demonstrating significant inhibitory activity. This compound exhibits anti-COVID-19 properties through its interaction with the main protease (Mpro), with an IC50 value of 30 nM. SDZ 224-015 is suitable for research applications focusing on inflammation, cytokine signaling, and viral pathogenesis.
  44. TNFα/IL-2 Inhibitor

    Immuno modulator-1 is a potent inhibitor of TNFα and IL-2, displaying IC50 values of 4.7 nM and 26 nM, respectively, in human peripheral blood mononuclear cells (hPBMC). This compound is valuable for investigating immune response modulation and inflammatory pathways. Additionally, Immuno modulator-1 demonstrates a hERG potassium channel blocking effect, exhibiting a 20% inhibitory percentage at a concentration of 3 μM, making it relevant for studies involving cardiac safety profiles.
  45. IL-13 Inhibitor

    IL13Rα2 D1 is a potent inhibitor of the IL-13/IL13Rα2 signaling pathway. It effectively suppresses IL-13-induced cellular processes, including adhesion, migration, invasion, and proliferation. Additionally, IL13Rα2 D1 inhibits the phosphorylation of key signaling proteins such as FAK, Src, AKT, and ERK1/2, as well as the expression of matrix metalloproteinases (MMPs). This compound is valuable for research focused on cancer biology, particularly in the context of colorectal cancer.
  46. NO、TNF-α、IL-12 Inhibitor

    (R)-5,7-Dimethoxyflavanone acts as an inhibitor of nitric oxide (NO), tumor necrosis factor-alpha (TNF-α), and interleukin-12 (IL-12), demonstrating significant anti-inflammatory properties. In biological assays, this compound exhibits potent antimutagenic activity, effectively reducing MeIQ-induced mutagenesis in the Ames test using S. typhimurium strains TA100 and TA98. Its capacity to modulate inflammatory mediators makes it a valuable tool in research focused on inflammation and mutagenesis.
  47. IL-1β Processing Inhibitor

    CP-424174 is a reversible inhibitor of IL-1β processing, acting with an IC50 of 210 nM. By indirectly inhibiting the NLRP3 inflammasome, CP-424174 plays a critical role in modulating inflammatory responses. This compound is useful for research applications focused on understanding the mechanisms of inflammation and potential therapeutic interventions in inflammatory diseases.
  48. Anti-PD-1 Antibody/IL-21 Mutein

    Latikafusp is a bifunctional fusion protein that functions as an anti-PD-1 antibody paired with an IL-21 mutein. This compound is designed to stimulate the IL-21 pathway specifically in PD-1+ cells, enhancing the priming and persistence of cytotoxic and memory T cells to promote anti-tumor immunity. Latikafusp is particularly relevant in research focused on solid tumors and has the potential to elicit immunogenicity-mediated responses.
  49. IL-17A Inhibitor

    LY3509754 is a potent IL-17A inhibitor, demonstrating IC50 values of less than 9.45 nM in alphaLISA assays and 9.3 nM in HT-29 cell assays. This compound's selective inhibition of IL-17A makes it a valuable tool for investigating the role of IL-17A in inflammatory diseases and immune responses. Its use in research applications can help elucidate the therapeutic potential for conditions associated with IL-17A signaling.
  50. IL-17A antagonist

    IL-17A antagonist 1 is a potent inhibitor of the interleukin-17A cytokine, demonstrating a binding affinity (Kd) of 0.66 μM and an inhibitory concentration (IC50) of 1.14 μM. This compound effectively modulates IL-17A signaling, making it a valuable tool for studying inflammatory responses and autoimmune disorders. It is suitable for research applications focused on understanding the role of IL-17A in various biological processes and therapeutic interventions.

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