IL Receptor

Resiniferatoxin ((+)-Resiniferatoxin) is a highly potent synthetic TRPV1 agonist that inhibits the production of Th1 cytokines and has anti-inflammatory activity, reducing serum levels of IL-12, INF-γ, IL-1β, TNF-α, NO, and PGE.

Dupilumab (REGN-668) is a fully human monoclonal antibody targeting the alpha subunit of the interleukin-4 receptor, thereby inhibiting IL-4 and IL-13 signaling. As a systemic immunomodulator, it has demonstrated efficacy in improving atopic dermatitis.

5-O-Caffeoylshikimic acid shows anti-oxidative activity; it also shows anti-inflammatory activity, the underlying mechanism was associated with downregulation of nuclear factor-κB.

Olamkicept (FE-301) is a soluble gp130-Fc-fusion protein that selectively inhibits interleukin 6 (IL-6) trans-signaling by binding to the soluble IL-6 receptor IL-6 complex.

Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory and immunosuppressive properties that induces autophagy and inhibits LPS-induced inflammatory responses in macrophages.

Secukinumab is a fully humanized monoclonal anti-IL-17A antibody and the first in its class to be approved by the US Food and Drug Administration for the treatment of moderate to severe plaque psoriasis.

Siltuximab(CNTO-328) is a monoclonal antibody with anti-tumor activity targeting IL-6 for the study of giant lymph node hyperplasia (MCD) and COVID-19.

Anakinra (Raleukin) is a cytokine inactivator and interleukin 1 receptor antagonist that can be used to study secondary phagocytic lymphohistiocytosis and rheumatoid arthritis.

Guselkumab (CNTO 1959) is a recombinant human IgG1 monoclonal antibody targeting the IL-23p19 subunit. Guselkumab binds to human cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol L, respectively. Guselkumab can inhibit the production of cytokines downstream of IL-23 signaling pathway, and can be used in the study of psoriatic arthritis.

Y-320 is a new phenylpyrazoleanilide immunomodulator.

IL-17A inhibitor 1 is a IL-17A inhibitor with IC50 of <9.45 nM in alphalisa assay. IL-17A inhibitor 1 inhibits HT-29 cells with IC50 of 9.3 nM.

Spesolimab (BI 655130) is an anti-interleukin-36 receptor antibody. It plays a crucial role in the immune system by reducing biomarkers associated with congenital Th1 Th17 and neutrophil pathways. Spesolimab can be used to study systemic pustular psoriasis, palmar and plantar impetigo (PPP), and atopic dermatitis.

Angoline (6-Methoxyldihydrochelerythrine) hydrochloride is a potent and selective IL6 STAT3 signaling pathway inhibitor(IC50 : 11.56 μM). It inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.

1. L-Arginine (L-Arg) exhibits anti-atherosclerotic effect. 2. L-Arginine and soy enriched diet are effective in prevention of osteoporosis associated with diabetes mellitus. 3. Exogenous L-Arginine could enhance neonate lymphocyte proliferation through an interleukin-2-independent pathway. 4. A combination of oral L-citrulline and L-Arginine effectively and rapidly augments NO-dependent responses at the acute stage.

Ac-YVAD-CMK (Ac-Tyr-Val-Ala-Asp-CMK) is a selective and irreversible inhibitor of Caspase-1 and inhibits pyroptosis, IL-1β and IL-18. Ac-YVAD-CMK shows neuroprotective and anti-inflammatory capacity.

Nothofagin has antioxidant, and antithrombotic activities, it possesses anti-inflammatory activity by inhibiting hyperpermeability, expression of CAMs, and adhesion and migration of leukocytes, thereby endorsing its usefulness as a therapy for vascular inflammatory diseases.

Benralizumab (MEDI-563) is a monoclonal antibody targeting the interleukin-5 receptor alpha (IL-5Rα). It enhances antibody-dependent cell-mediated cytotoxicity, leading to a rapid depletion of eosinophils. Benralizumab is used for severe eosinophilic asthma and can be employed to prevent exacerbations of chronic obstructive pulmonary disease.

Apilimod (STA 5326) inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis.

PF-07038124 HCl is a selective and potent PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2.PF-07038124 HCl inhibits IL-13, IL-4, and IFNγ, and can be used in the study of skin disorders such as atopic dermatitis and plaque psoriasis.

1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res

AF 12198 Acetate is a novel low molecular weight antagonist of IL-1

Elubrixin (SB-656933) inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation. Elubrixin is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist.

BIRT-377 is a negative allosteric and orally bioavailable inhibitor of ICAM-1 and LFA-1(Ki = 25.8 nM). BIRT-377 inhibits the production of IL-2 and can be used in studies about inflammatory and immune disorders.

1. Berberrubine chloride (9-Berberoline Chloride) has antitumor activity. 2. Berberrubine has antidiabetic activity. 3. Berberrubine dose-dependently inhibits IL-8 and MCP-1 protein levels in the media and mRNA expression of the cells stimulated with IL-1beta or TNF-alpha.

Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin is also an effective reversal agent for the multidrug resistance of tu

Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.

Taraxasterol (Taraxasterin) is compound with anti-inflammatory activity.

Apilimod 2HCl (STA 5326 2HCl) is a PIKFYVE kinase inhibitor that promotes NLRP3 inflammatory vesicle activation, IL-1β secretion, and cellular pyroptosis, and is used in the study of amyotrophic lateral sclerosis.

Brodalumab (AMG 827) is a human monoclonal IgG2 antibody targeting the interleukin 17 receptor (IL-17R), commonly used as an immunosuppressant in treating psoriasis.

Ixekizumab (LY2439821) is a humanized IgG4 monoclonal antibody that selectively binds and neutralizes interleukin IL-17A with a Kd value of <3 pM. It blocks the binding of IL-17A to IL-17RA but not to other IL-17 family members. Ixekizumab is used for the treatment of moderate to severe plaque psoriasis, psoriasis, arthritis, and psoriasis.

Netakimab (BCD 085) is a humanized camel-derived monoclonal antibody targeting interleukin-17A, which can be used to study spondyloarthritis and plaque psoriasis.

1. Negletein (7-O-Methylbaicalein) has anti-inflammatory and immunomodulatory activities via inhibition of TNF-α, iNOS and IL-1β. 2. Negletein as a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells. 3. Negletein shows a comparable redox-active potential, and it (50 μM, 4 h) can activate Nrf2. 4. Negletein shows significant antimicrobial activity. 5. Negletein has anti-hypoxia activity, it can significantly prolong the survival time of hypoxic mice.6. Negletein has anti- Alzheimer's disease activity, it inhibits the iron-dependent formation of ROS and also blocks the iron-induced oligomerization of amyloid beta 42 in vitro. 7. Negletein (IC50: 3.89 + - 0.39 microM) exhibits potent inhibitory activity against nuclear factor of activated T cells (NFAT) transcription factor.

Risankizumab (BI 655066) is a humanized IgG monoclonal antibody (Kd <10 pM) targeting the IL-23 p19 subunit. It inhibits IL-17 production induced by human IL-23 in mouse splenocytes with an IC50 value of 2 pM. Risankizumab is used for the prevention and treatment of immune and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis, and erythrodermic psoriasis.

Xeligekimab (GR 1501) is a fully human monoclonal antibody that selectively neutralizes IL-17A, has potential anti-inflammatory activity, and can be used to study plaque psoriasis.

Vunakizumab (Anti-Human IL17A Recombinant Antibody) is a human IgGκ monoclonal antibody that specifically targets and inhibits IL-17A's receptor interaction, making it useful for researching autoimmune conditions such as psoriatic arthritis, ankylosing spondylitis, multiple sclerosis, and inflammatory arthritis [1].

Kuwanon E, a flavonoid obtained from Morus alba, has potential anti-inflammatory activity, inhibits TNF-α and IL-1β secretion, and suppresses NF-κB nuclear translocation in LPS-stimulated macrophages.

HuMax-IL8 (MDX 018) is a humanized anti-IL-8 monoclonal antibody for the study of metastatic or unresectable solid tumors.

BI605906 is an IKKβ inhibitor that inhibits tumor necrosis factor alpha-dependent IkappaB degradation and expression of the pro-inflammatory mediator interleukin-6, which can be used to study inflammatory skin diseases such as psoriasis.

Pranlukast (ONO-1078) is a cysteinyl leukotriene receptor-1 antagonist. It antagonizes or reduces bronchospasm caused, principally in asthmatics, by an allergic reaction to accidentally or inadvertently encountered allergens.

Aucubin (Rhinanthin) is an iridoid glycoside with anti-inflammatory, anti-microbial, anti-algesic as well as anti-tumor activities.

Canakinumab (ACZ885) is a recombinant human IL-1β-targeting monoclonal antibody that inhibits human and chorioallantoic monkey IL-1β with IC50 values of 43.6 and 40.8 pM, respectively. It exhibits anti-inflammatory activity by neutralizing IL-1β signaling, and it has been used for the treatment of gout and coronary artery disease.

IL-4 inhibitor is an inhibitor of IL-4.1It binds to IL-4 with a Kdvalue of 1.8 μM and inhibits IL-4 activity in a cell-based reporter assay (EC50= 1.81 μM). It is selective for IL-4 over IL-13 (EC50= 18.2 μM). IL-4 inhibitor inhibits IL-4-induced STAT6 phosphorylation in THP-1 monocytes (EC50= 3.1 μM), indicating inhibition of the IL-4-JAK1-STAT6 signaling pathway.

Apilimod mesylate (STA 5326 mesylate) is a potent IL-12 IL-23 inhibitor.

Shanziside (Shanzhiside) has immunosuppressive activity, it shows significant inhibition of IL-2 secretion by phorbol myristate acetate and anti-CD28 monoclonal antibody co-stimulated activation of human peripheral blood T cells.

Mogroside IIe is a bitter triterpenoid saponin which is the main component of unripe Luo Han Guo fruit and a precursor of the commercially available sweetener mogroside V.

Vopikitug is a humanized monoclonal antibody targeting IL-2RA with antitumor activity. It can be used to study cancer.

LMT-28 is an inhibitor of IL-6 and selectively inhibits IL-6-induced phosphorylation of gp130, STAT3, and JAK2.

Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.