interleukin (il)6 receptor

Interleukin (IL)-6 Receptor, a peptide, binds to IL-6 facilitating signal transduction and playing a crucial role in inflammatory and immune responses.

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.

Tocilizumab (Anti-Human IL6R) is a neutralizing antibody against human interleukin-6 receptor (IL-6R) that blocks the binding of IL-6 to IL-6R, thereby inhibiting both classical and trans signaling. It can be used to study rheumatoid arthritis and has been suggested as a possible drug for the treatment of severe COVID-19.

Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities.

Muscone (3-Methylcyclopentadecanone) is an organic compound that is the primary contributor to the odor of musk.

Hydrocortisone hemisuccinate (hydrocortisone 21-hemisuccinate*free acid) is a corticosteroid used as an analytical and chromatography reagent.

Triamcinolone (Aristocort) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.

RV01 is a novel quinoline-substituted analogue of resveratrol that inhibits DNA damage, reduces ethanol-induced acetaldehyde dehydrogenase (ALDH2) mRNA expression, and has hydroxyl radical scavenging activity. rV01 reduces iNOS expression and has anti-neuroinflammatory effects. rV01 reduces tumor necrosis factor-a (TNF-a) and interleukin-6 (IL-6) mRNA levels and secretion. RV01 reduced tumor necrosis factor-a (TNF-a) and interleukin-6 (IL-6) mRNA levels and secretion, inhibited lps-induced ROS production and nicotinamide adenine dinucleotide phosphate (NADPH) oxidase activation, decreased toll-like receptor 4 (TLR4) protein expression, and inhibited lps-induced activation of mitogen-activated protein kinase (MAPK) and nuclear transcription factor-кB (NF-кB) signaling pathways.

Glucocorticoid receptor/NF-κB modulator-1 (Compound 20) is a derivative of ocotillol. It prevents degradation of glucocorticoid receptor (GR) mRNA and GR protein and inhibits the activation of the NF-κB signaling pathway. Additionally, it reduces levels of nitric oxide (NO), interleukin (IL-6), and tumor necrosis factor-alpha (TNF-α), and improves sepsis in mice.

ST-899 is an innovative platelet-activating factor (PAF) receptor antagonist. It significantly reduces the mortality rate in mice experiencing shock induced by endotoxins (LPS). The compound markedly inhibits the LPS-induced increase in serum tumor necrosis factor (TNF) levels while leaving interleukin-6 (IL-6) unaffected. The mechanism by which ST-899 operates involves disrupting the positive feedback loop between PAF and TNF, thereby mitigating inflammatory responses. ST-899 is applicable for studies related to inflammatory diseases such as septic shock.

Diflorasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. Like other glucocorticoids, diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm

Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminomethyl)benzamide) is the analogue of BMS-509744, which can potently and selectively inhibit Itk kinase activity. In vitro: BMS-509744 could reduce TCR-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells [1]. In vivo: BMS-509744 suppressed the production of IL-2 induced by anti-TCR antibody administered to mice. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma [1]. Clinical trial: Up to now, both BMS-509744 and ITK inhibitor is still in the preclinical development stage.

Kansuinine B inhibits Stat3 activation induced by IL-6. Kansuinine B exhibits anti-viral activity and could be used in COVID-19 research.

AX-024 hydrochloride (AX-024 HCl) is an cytokine release inhibitor which can strongly inhibit the production of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10 and IL-17A.

IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor-associated kinase 4 [IRAK-4, IC50: 160 nM].

Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.

GNE-2256 (molecule 19) is an orally active inhibitor of interleukin-1 receptor–associated kinase 4 (IRAK4) with a binding affinity of 1.4 nM and an IL-6 IC50 value of 190 nM, making it a valuable research compound for studying inflammatory signaling cascades, innate immune responses, and cytokine-driven pathological processes.

Clazakizumab is a humanized monoclonal antibody targeting human interleukin -6(IL-6) with high affinity. By directly binding IL-6 ligand, it blocks its interaction with IL-6 receptor (IL-6α) and signal co-receptor gp130, thus inhibiting the activation of downstream JAK/STAT signaling pathway and weakening the inflammatory response. Clazakizumab can be used in the study of psoriasis arthritis and antibody-mediated organ transplant rejection.

Sarilumab (SAR-153191)is a potent interleukin-6 IL-6 receptor antagonist and a human immunoglobulin G1 monoclonal antibody. Sarilumab inhibits IL-6-mediated signaling and reduces inflammation.Sarilumab is used for the prevention and treatment of rheumatoid arthritis.

Ziltivekimab (MEDI 5117) is a CHO-expressed humanized monoclonal antibody targeting IL-6/IFNb2 for use in immune system diseases.

Diflorasone (Standard) is the standard substance of Diflorasone, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Diflorasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. Like other glucocorticoids, diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm. The receptor complex subsequently translocates to the nucleus and activates or represses genes by interacting with short, palindromic DNA sequences called glucocorticoid response element (GRE). Gene activation leads to the exertion of anti-inflammatory effects, e.g. upregulation of IkappaB, while gene repression inhibits production of pro-inflammatory cytokines such as interleukin-1 (IL-1), IL-2 and IL-6, thereby preventing activation of cytotoxic T-lymphocytes.

Triamcinolone (Standard) is the standard substance of Triamcinolone, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Triamcinolone (Aristocort) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.

Kansuinine A possesses analgesic props, it also shows NGF inducing activity.