IL Receptor

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.

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.

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.

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.

Y-320 is a new phenylpyrazoleanilide immunomodulator.

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.

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.

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.

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

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.

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.

Tralokinumab is a fully human IgG4 monoclonal antibody with a high affinity for IL-13 alone. Tralokinumab's potential anti-inflammatory activity prevents IL-13 receptor interaction and subsequent downstream signaling and can be used to study atopic dermatitis (AD).

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

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.

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.

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

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.

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

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.

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.

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.

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. 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.

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

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

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.

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

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.

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.

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.

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

SDZ 224-015 is an orally active inhibitor of interleukin-1β (IL-1β) converting enzyme and caspase-1, exhibiting anti-COVID-19 and anti-inflammatory activity, and reducing carrageenan gum-induced paw edema in rats.

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.

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.

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.

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

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.

Inosine pranobex (Delimmun) has a number of immunomodulatory effects, including inducing T-lymphocyte differentiation, augmenting macrophage and NK cell functions, and stimulating IL-2 production. Through these effects and others, isoprinosine shows antiviral activity and has applications against subacute sclerosing panencephalitis. It also restores depressed immune responses in Y patients after irradiation and reduces the incidence of infection in leukemia patients undergoing chemotherapy. It is most commonly used to treat the rare measles complication subacute sclerosing panencephalitis in conjunction with intrathecal interferon therapy.

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

Lusvertikimab (OSE-127) is a humanized anti-IL7R antibody with anti-leukemic efficacy that reduces leukemic load in xenograft ALL through antibody-dependent phagocytosis and may be used to study leukemia.

Hispidulin 7-glucuronide is a flavonoid that can be extracted from the leaves of mistletoe and has potential anti-inflammatory activity, inhibiting the release of IL-6.

Moringin is an isothiocyanate obtained from myrosinase-mediated hydrolysis of the glucosinolate precursor glucoMoringin present in Moringa oleifera seeds. Moringin has anti-inflammatory and antioxidative properties.

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.

Protosappanin A (PTA) has anti-oxidative nitrative activities on brain immune and neuroinflammation through regulation of CD14 TLR4-dependent IKK IκB NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.