IL-6
IL-6 is a pleiotropic cytokine that regulates immune response, acute inflammation, tissue regeneration, metabolism, and stromal activation[1][2]. Mechanistically, IL-6 binds IL-6Rα and recruits gp130, activating JAK/STAT3 signaling and downstream transcriptional programs[1][3]. Disease relevance depends strongly on receptor context: membrane IL-6Rα supports classic signaling, whereas soluble IL-6Rα enables trans-signaling in gp130-expressing cells and drives pro-inflammatory activity[1][4]. Compared with these receptor forms, gp130 is broadly expressed, while IL-6R expression is restricted to selected cells such as hepatocytes and leukocytes, explaining cell-type-selective responsiveness[1]. In vascular endothelial cells, IL-6 trans-signaling induces MCP-1 through coordinated JAK/STAT3 and PI3K/AKT activation[5]. In proliferative vitreoretinopathy models, IL-6 promotes retinal pigment epithelial proliferation and epithelial-mesenchymal transition through JAK1/STAT3 signaling[6]. For experimental intervention, tocilizumab, a humanized anti-IL-6R antibody, blocks IL-6 signaling and improves rheumatoid arthritis outcomes in controlled clinical studies[7][8].
References:
- [1]. Rose-John S. IL-6 trans-signaling via the soluble IL-6 receptor: importance for the pro-inflammatory activities of IL-6. Int J Biol Sci. 2012;8(9):1237-47. doi: 10.7150/ijbs.4989. Epub 2012 Oct 24. PMID: 23136552; PMCID: PMC3491447. et al. IL-6 trans-signaling via the soluble IL-6 receptor: importance for the pro-inflammatory activities of IL-6. Int J Biol Sci. 2012;8(9):1237-47. [Content Brief]
- [2]. Danese S, et al. Interleukin-6: a therapeutic Jekyll and Hyde in gastrointestinal and hepatic diseases. Gut. 2010 Feb;59(2):149-51. [Content Brief]
- [3]. Reeh H, et al. Response to IL-6 trans- and IL-6 classic signalling is determined by the ratio of the IL-6 receptor α to gp130 expression: fusing experimental insights and dynamic modelling. Cell Commun Signal. 2019 May 17;17(1):46. [Content Brief]
- [4]. Maes M, et al. Targeting classical IL-6 signalling or IL-6 trans-signalling in depression? Expert Opin Ther Targets. 2014 May;18(5):495-512. [Content Brief]
- [5]. Zegeye MM, et al. Activation of the JAK/STAT3 and PI3K/AKT pathways are crucial for IL-6 trans-signaling-mediated pro-inflammatory response in human vascular endothelial cells. Cell Commun Signal. 2018 Sep 5;16(1):55. [Content Brief]
- [6]. Chen X, et al. Interleukin-6 promotes proliferative vitreoretinopathy by inducing epithelial-mesenchymal transition via the JAK1/STAT3 signaling pathway. Mol Vis. 2020 Jul 29;26:517-529. [Content Brief]
- [7]. Ohsugi Y, et al. The recombinant humanized anti-IL-6 receptor antibody tocilizumab, an innovative drug for the treatment of rheumatoid arthritis. Expert Opin Biol Ther. 2008 May;8(5):669-81. [Content Brief]
- [8]. Emery P, et al. IL-6 receptor inhibition with tocilizumab improves treatment outcomes in patients with rheumatoid arthritis refractory to anti-tumour necrosis factor biologicals: results from a 24-week multicentre randomised placebo-controlled trial. Ann Rheum Dis. 2008 Nov;67(11):1516-23. [Content Brief]
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Recombinant Proteins (24)
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Xelafaslatide
0 ImagesSynonyms: ONL-1204Xelafaslatide (ONL-1204) is a Fas receptor antagonist. Xelafaslatide blocks the Fas receptor signaling pathway and inhibits downstream apoptosis and inflammatory pathways. Xelafaslatide suppresses neuroinflammation and microglial activation in glaucoma models, protects retinal ganglion cells and prevents axonal degeneration. Xelafaslatide is applicable to relevant research on glaucoma.
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Hordenine
0 ImagesHordenine (Ordenina; Peyocactine) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.
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Bivalirudin TFA
0 ImagesBivalirudin TFA, a hirudin analog and anticoagulant, is a direct thrombin inhibitor. Bivalirudin TFA inhibits thrombin-mediated fibrinogen cleavage, coagulation factor activation, and platelet activation by reversibly binding to thrombin. In addition, Bivalirudin TFA also has certain effects of anti-virus, anti-inflammation, and vascular endothelial barrier function protection. Bivalirudin TFA can be used for the research of thrombotic diseases and others.
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Militarine
0 ImagesMilitarine is a plant growth inhibitor and anti-inflammatory agent. Militarine inhibits the elongation of radicles and hypocotyls in seedlings of lettuce, Italian ryegrass and timothy grass. Militarine alleviates PM2.5-induced inflammatory injury and inhibits cell migration in human alveolar epithelial A549 cells by inhibiting the NF-κB signaling pathway, reducing oxidative stress and the release of inflammatory factors. Militarine can be used in studies related to PM2.5-induced pulmonary diseases.
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ADP-β-S trilithium
0 ImagesCat. No.: HY-134353BCAS No.: 73536-95-5Synonyms: Adenosine 5'-β-thiodiphosphate trilithiumADP-β-S (Adenosine 5'-(β-thiodiphosphate)) trilithium is a non-hydrolyzable ADP analog and a P2Y12 receptor agonist. ADP-β-S trilithium activates the P2Y12 receptor in microglia, thereby triggering downstream inflammatory signaling pathways. ADP-β-S trilithium activates P2Y purinergic receptors in rat pancreatic β cells and enhances glucose-induced insulin secretion. ADP-β-S trilithium can be used in the research of diseases such as inflammation and diabetes.
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Piperonylic acid
0 ImagesPiperonylic acid is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic Acid is a selective, mechanism-based inactivator of the trans-cinnamate 4-Hydroxylase. Piperonylic acid has anticancer, antioxidant and antibacterial activities.
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Phellodendrine chloride
0 ImagesPhellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.
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Adrenocorticotropic hormone TFA
0 ImagesCat. No.: HY-106373APurity: 99.91%Synonyms: ACTH TFA; Adrenocorticotrophic hormone TFAAdrenocorticotropic hormone (ACTH; Adrenocorticotrophic hormone) TFA is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone TFA stimulates cortisol secretion from the adrenal cortex via the hypothalamic-pituitary-adrenal (HPA) axis. Adrenocorticotropic hormone TFA regulates cortisol and androgen production. Adrenocorticotropic hormone TFA can promote the development of spermatogenesis. Adrenocorticotropic hormone TFA can relieve acute inflammation in gout models by inhibiting the polarization of macrophages to M1 type, inhibiting ROS and proinflammatory factor production and protecting mitochondrial function. Adrenocorticotropic hormone TFA can be used for the researches of inflammation, endocrinology, metabolic disease, such as gout and nephrotic syndrome.
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Gamma-glutamylcysteine TFA
0 ImagesCat. No.: HY-113402ACAS No.: 283159-88-6Synonyms: γ-Glu-Cys TFAGamma-glutamylcysteine TFA (γ-Glu-Cys TFA) is an orally active, blood-brain barrier permeable dipeptide. Gamma-glutamylcysteine TFA activates AMPK, SIRT1, IL-4/STAT6, AC/cAMP/PI3K, IGF-1R/IRS1/PI3K, and Nrf2 signaling pathways; it inhibits NF-κB, JAK1/STAT1/3, MAPKs, cadmium-induced p38 MAPK, JNK, and PI3K/Akt signaling pathways. Gamma-glutamylcysteine TFA regulates macrophage polarization, modulates the trafficking of CD36 and GLUT4, induces glutathione synthesis, improves metabolic dysfunction, reduces lipid deposition, ameliorates glucose homeostasis, inhibits apoptosis (Apoptosis), stabilizes mitochondria, suppresses lipid peroxidation, iron accumulation and ferroptosis (Ferroptosis), reduces ds-HMGB1 levels, reverses mechanical hyperalgesia, and alleviates hepatic lipid droplet formation. Gamma-glutamylcysteine TFA is applicable to research related to inflammatory bowel disease, type 2 diabetes, cadmium-induced neurotoxicity, Alzheimer's disease, cerebral ischemia/reperfusion injury, neuropathy, and alcoholic liver disease.
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TMI-1
0 ImagesSynonyms: WAY-171318TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions.
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DL-Tryptophan
0 ImagesSynonyms: (±)-TryptophanDL-Tryptophan ((±)-Tryptophan) is an orally effective aryl hydrocarbon receptor (AhR) agonist. DL-Tryptophan reduces the expression of pro-inflammatory cytokines IL-6, TNF-α, IL-1β, as well as liver injury markers aspartate aminotransferase and alanine aminotransferase, and alleviates hepatocyte apoptosis (apoptosis) in sepsis induced by cecal ligation and puncture. DL-Tryptophan can be used in the research of sepsis-related acute liver injury.
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Gomisin N
0 ImagesGomisin N is an orally active lignan compound. Gomisin N can be isolated from Schisandra chinensis. Gomisin N induces Apoptosis in a variety of cells. Gomisin N activates AMPK, Akt, MAPK/ERK, Nrf2, caspase-3 and PARP-1. Gomisin N inhibits GSK3β, nitric oxide (NO), and proinflammatory cytokines (IL-1β, IL-6, TNF-α). Gomisin N has anti-inflammatory, antioxidant, anti-obesity, anti-diabetic, and anti-melanogenesis activities. Gomisin N has anti-tumor activity against cervical cancer and liver cancer. Gomisin N improves Alzheimer's disease.
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RCGD423
0 ImagesRCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.
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Artemisic acid
0 ImagesSynonyms: Qing Hao acid; Artemisinic acid; Arteannuic acidArtemisinic acid (Qing Hao acid) is a sesquiterpene that can be isolated from Artemisia annua L. Artemisinic acid is also an important precursor for the synthesis of Artemisinin (HY-B0094). Artemisinic acid has various pharmacological activities, such as antimalarial activity, antitumor activity, antipyretic effect, antibacterial activity, allelopathic effect, and anti-adipogenic effect.
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Broussonin E
0 ImagesBroussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis.
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(20R)-Protopanaxadiol
0 Images(20R)-Protopanaxadiol is a metabolite of ginsenosides. (20R)-Protopanaxadiol has anti-inflammatory and antibacterial activities, but shows no significant cytotoxicity against tumor cell lines. In addition, (20R)-Protopanaxadiol can inhibit the uptake of 2-deoxy-D-glucose (2-DG).
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Carveol
0 ImagesCarveol is an orally active monoterpenoid alcohol with neuroprotective, antioxidant, anti-inflammatory, anticonvulsant, antidiabetic, hypolipidemic and hepatoprotective activities. Carveol upregulates the expression of Bcl2, downregulates the expression of caspase-3, TNF-α, IL1β and IL6, activates the Nrf2/HO-1 antioxidant signaling pathway, inhibits the RAGE/NF-κB signaling pathway, and suppresses neuroinflammation and neuronal apoptosis. Carveol inhibits α-synuclein aggregation, improves cognitive ability, and inhibits α-amylase activity. Carveol exerts neuroprotective effects in a rat model of Parkinson's disease. Carveol exhibits antidiabetic effects in alloxan-induced diabetic rats. Carveol alleviates PTZ-induced seizures in rats. Carveol can be used in research related to Parkinson's disease, epilepsy, diabetes and ischemic stroke.
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WWL229
0 ImagesWWL229 is a selective inhibitor of carboxylesterase 3 (CES3) with an IC50 1.94 μM. WWL229 attenuates LPS (HY-D1056)-induced pro-inflammatory cytokine mRNA levels, inhibits lipolysis and adipose thermogenesis, impairs mitochondrial function, and promotes lipid storage. WWL229 can be used for the research of obesity, insulin resistance, type 2 diabetes, and lung inflammation.
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Parishin C
0 ImagesParishin C is a brain-penetrant major bioactive component found in Gastrodia elata Blume. Parishin C is a 5-HT1A receptor agonist with an EC50 of 34 nM. Parishin C has antipsychotic and neuroprotective effects. Parishin C protects against Aβ-induced long-term potentiation damage and NMDA receptor current impairment. Parishin C reduces oxidative stress, pro-inflammatory cytokine levels, caspase activity, brain water content, and cerebral infarct volume; increases antioxidant enzyme activity and BDNF levels; improves nerve function and histopathological brain damage. Parishin C attenuates phencyclidine-induced immobility time increases, sociability deficits, and visual recognition memory impairment. Parishin C can be used for the research of ischemic stroke, Alzheimer's disease, and schizophrenia-like psychosis.
