1. Signaling Pathways
  2. Apoptosis
  3. TNF Receptor

TNF Receptor

Tumor Necrosis Factor Receptor; TNFR

Tumor necrosis factor (TNF) is a major mediator of apoptosis as well as inflammation and immunity, and it has been implicated in the pathogenesis of a wide spectrum of human diseases, including sepsis, diabetes, cancer, osteoporosis, multiple sclerosis, rheumatoid arthritis, and inflammatory bowel diseases.

TNF-α is a 17-kDa protein consisting of 157 amino acids that is a homotrimer in solution. In humans, the gene is mapped to chromosome 6. Its bioactivity is mainly regulated by soluble TNF-α–binding receptors. TNF-α is mainly produced by activated macrophages, T lymphocytes, and natural killer cells. Lower expression is known for a variety of other cells, including fibroblasts, smooth muscle cells, and tumor cells. In cells, TNF-α is synthesized as pro-TNF (26 kDa), which is membrane-bound and is released upon cleavage of its pro domain by TNF-converting enzyme (TACE).

Many of the TNF-induced cellular responses are mediated by either one of the two TNF receptors, TNF-R1 and TNF-R2, both of which belong to the TNF receptor super-family. In response to TNF treatment, the transcription factor NF-κB and MAP kinases, including ERK, p38 and JNK, are activated in most types of cells and, in some cases, apoptosis or necrosis could also be induced. However, induction of apoptosis or necrosis is mainly achieved through TNFR1, which is also known as a death receptor. Activation of the NF-κB and MAPKs plays an important role in the induction of many cytokines and immune-regulatory proteins and is pivotal for many inflammatory responses.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-176882
    ASK1-IN-11
    Inhibitor
    ASK1-IN-11 (Compound 7) is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 <200 nM. ASK1-IN-11 also shows inhibitory activities to TNF-α, MYLK/MLCK Kinase and hERG potassium channels . ASK1-IN-11 can be used for the research of inflammation.
    ASK1-IN-11
  • HY-168935
    Anti-inflammatory agent 95
    Inhibitor
    Anti-inflammatory agent 95 (Compound 2e) is an anti-inflammatory agent that exhibits the most potent anti-inflammatory activity in LPS (HY-D1056)-induced RAW 264.7 mouse macrophages. It significantly inhibits the production of NO, with an IC50 of 8.8 μM, and reduces the secretion of TNF-α and IL-1β, with inhibition rates reaching 60% and over 90%, respectively, at a concentration of 100 μM. Anti-inflammatory agent 95 holds promise for research in the field of inflammatory diseases.
    Anti-inflammatory agent 95
  • HY-N0507R
    Rosavin (Standard)
    Inhibitor
    Rosavin (Standard) is the analytical standard of Rosavin. This product is intended for research and analytical applications. Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis.
    Rosavin (Standard)
  • HY-N0261R
    Aurantio-obtusin (Standard)
    Inhibitor
    Aurantio-obtusin (Standard) is the analytical standard of Aurantio-obtusin. This product is intended for research and analytical applications. Aurantio-obtusin is a anthraquinone compound that can be extracted from cassia seed. Aurantio-obtusin has the effects of decreasing blood pressure, decreasing blood lipids and anti-inflammatory.Aurantio-obtusin is an orally active vasodilator. Aurantio-obtusin ameliorates hepatic steatosis through AMPK/ autophagy-and AMPK/TFEB mediated inhibition of lipid accumulation.
    Aurantio-obtusin (Standard)
  • HY-N16527
    7-O-Galloyl-D-sedoheptulose
    Inhibitor
    7-O-Galloyl-D-sedoheptulose is an orally effective polyphenolic compound. 7-O-Galloyl-D-sedoheptulose lowers the serum levels of glucose, leptin, insulin, C-peptide, resistin, TNF-α, IL-6, and increases the serum level of adiponectin. 7-O-Galloyl-D-sedoheptulose significantly reduces the levels of ROS and lipid peroxidation products (TBARS) by down-regulating the protein expression of NADPH oxidase subunit Nox-4 and p22phox. 7-O-Galloyl-D-sedoheptulose down-regulates NF-κB and related pro-inflammatory factors (COX-2, iNOS), inhibits the phosphorylation of JNK and the activity of its downstream AP-1. 7-O-Galloyl-D-sedoheptulose reduces the expression of TGF-β1 and fibronectin, indicating its potential in anti-tissue fibrosis. 7-O-Galloyl-D-sedoheptulose can be used for the study of type 2 diabetes and its hepatic and pancreatic complications.
    7-O-Galloyl-D-sedoheptulose
  • HY-182026
    FXR agonist 17
    Inhibitor
    FXR agonist 17 is an orally active, steroidal FXR agonist with EC50 values of 42.2 nM (TR-FRET) and 176.4 nM (luciferase reporter assay), respectively. FXR agonist 17 activates TGR5 (EC50 = 2.6 μM) but does not activate hMRGPRX4. FXR agonist 17 exerts anti-inflammatory, hepatoprotective and antifibrotic effects, improves the non-alcoholic steatohepatitis (NAFLD) activity score and reduces the severity of liver fibrosis. FXR agonist 17 can be used for the research of NAFLD, cholestatic liver disease and liver fibrosis.
    FXR agonist 17
  • HY-P10693
    CZEN-002
    Inhibitor
    CZEN-002 is a derivative of alpha-melanocyte-stimulating hormone that has anti-inflammatory and antibacterial properties, inhibiting the production of TNF-α.
    CZEN-002
  • HY-178240
    rel-(1S,2R)-Dihydro bupropion
    Inhibitor
    rel-(1S,2R)-Dihydro bupropion is a metabolite of bupropion. rel-(1S,2R)-Dihydro bupropion can promote endogenous IL-10 production and inhibit Th1 cytokines (IL-12 and TNF-α). rel-(1S,2R)-Dihydro bupropion can induce immune response transition from Th1 to Th2. rel-(1S,2R)-Dihydro bupropion can be used for research on inflammatory conditions.
    rel-(1S,2R)-Dihydro bupropion
  • HY-P991553
    HeFi-1
    Inhibitor
    HeFi-1 is a mouse anti-CD30 IgG1 monoclonal antibody. HeFi-1 recognizes the ligand-binding site on CD30. HeFi-1 can inhibit the growth of tumor cells with high expression of CD30. HeFi-1 can induce eosinophil apoptosis. HeFi-1 can be used for researches on cancer or inflammation conditions such as anaplastic large-cell lymphoma (ALCL) and asthma.
    HeFi-1
  • HY-123568
    PBI-1393
    Inhibitor
    PBI-1393 (BCH-1393) is an anticancer agent that enhances Th1 type cytokine production and primary T cell activation.
    PBI-1393
  • HY-144727
    Anti-inflammatory agent 11
    Inhibitor
    Anti-inflammatory agent 11 (compound 16) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 11 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 1.3 and 6.9 μM, respectively. Anti-inflammatory agent 11 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 11 can be used for tuberculosis (TB) research.
    Anti-inflammatory agent 11
  • HY-181248
    BChE-IN-49
    Inhibitor
    BChE-IN-49 is an orally active BChE inhibitor with IC50 values of 0.73 μM and 6.43 μM against BChE and AChE, respectively. BChE-IN-49 reduces AChE levels to inhibit the degradation of acetylcholine. By inhibiting GSK-3β, BChE-IN-49 potently activates the Wnt/β-catenin signaling pathway, exerting potent anti-, antioxidant, anti-neuroinflammatory and anti-apoptotic effects. BChE-IN-49 can be used in research related to Alzheimer's disease.
    BChE-IN-49
  • HY-183367
    Anti-inflammatory agent 115
    Inhibitor
    Anti-inflammatory agent 115 is a potent anti-inflammatory agent. Anti-inflammatory agent 115 reduces secretion of myeloperoxidase (MPO), TNF-α, IL-1β, and IL-6. Anti-inflammatory agent 115 decreases ear tissue thickness and neutrophil infiltration in 12-O-tetradecanoylphorbol-13-acetate (TPA) (HY-18739)-induced topical edema in mice. Anti-inflammatory agent 115 can be used for the research of inflammatory diseases.
    Anti-inflammatory agent 115
  • HY-106215
    Etiprednol dicloacetate
    Inhibitor
    Etiprednol dicloacetate (BNP 166) is an anti-inflammatory agent. Etiprednol dicloacetate inhibits eosinophil accumulation. Etiprednol dicloacetate can be used in the research of inflammatory airway diseases, such as asthma.
    Etiprednol dicloacetate
  • HY-W709413
    Panaxytriol
    Inhibitor
    Panaxytriol is an active component of ginseng. Panaxytriol inhibits the nuclear translocation of NF-κB, thereby reducing the production of pro-inflammatory factors (such as TNF-α, IL-1β, IL-6) and nitric oxide (NO) induced by LPS (HY-D1056). Panaxytriol upregulates CYP3A4 by activating the nuclear receptor PXR/CAR. Panaxytriol improves motor dysfunction in a mouse model of brain inflammation. Panaxytriol can be used in the research of neurodegenerative diseases (such as Alzheimer's disease).
    Panaxytriol
  • HY-123670
    RPR-200765A methanesulfonate
    Inhibitor
    RPR-200765A methanesulfonate is an orally active p38 MAPK inhibitor with an IC50 of 0.050 μM. RPR-200765A methanesulfonate shows weak activity against Lck, and exhibits no significant activity against ERK, ZAP70 or SYK. It inhibits the production of TNFα and can be used in the research of inflammatory diseases.
    RPR-200765A methanesulfonate
  • HY-N0604R
    Ginsenoside Rh1 (Standard)
    Inhibitor
    Ginsenoside Rh1 (Standard) is the analytical standard of Ginsenoside Rh1. This product is intended for research and analytical applications. Ginsenoside Rh1 (Prosapogenin A2) inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
    Ginsenoside Rh1 (Standard)
  • HY-157809
    Anti-inflammatory agent 74
    Inhibitor
    Anti-inflammatory agent 74 (B5) is an anti-inflammatory agent that can inhibit NO, IL-6, and TNF-α, with IC50 values of 10.88 μM and 4.93 μM for NO and IL-6, respectively. Anti-inflammatory agent 74 alleviates acute lung injury (ALI) by regulating inflammatory mediators and inhibiting the MAPK and NF-κB signaling pathways.
    Anti-inflammatory agent 74
  • HY-149816
    Anti-inflammatory agent 41
    Inhibitor
    Anti-inflammatory agent 41 (13a) significantly inhibit lipopolysaccharide (LPS)-induced expression of the proinflammatory cytokines IL-6 and TNF-α on J774A.1, THP-1 and LX-2 cells, and inhibits the activation of the NF-κB pathway.
    Anti-inflammatory agent 41
  • HY-N15519
    Crocatin B
    Inhibitor
    Crocatin B is found in P. crocatum Ruiz & Pav. Crocatin B exerts anti-inflammatory activity by inhibiting the expression of TNF-α and ICAM-1. Crocatin B has anti-tumor activity.
    Crocatin B
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

Following the binding of TNF to TNF receptors, TNFR1 binds to TRADD, which recruits RIPK1, TRAF2/5 and cIAP1/2 to form TNFR1 signaling complex I; TNFR2 binds to TRAF1/2 directly to recruit cIAP1/2. Both cIAP1 and cIAP2 are E3 ubiquitin ligases that add K63 linked polyubiquitin chains to RIPK1 and other components of the signaling complex. The ubiquitin ligase activity of the cIAPs is needed to recruit the LUBAC, which adds M1 linked linear polyubiquitin chains to RIPK1. K63 polyubiquitylated RIPK1 recruits TAB2, TAB3 and TAK1, which activate signaling mediated by JNK and p38, as well as the IκB kinase complex. The IKK complex then activates NF-κB signaling, which leads to the transcription of anti-apoptotic factors-such as FLIP and Bcl-XL-that promote cell survival. 

 

The formation of TNFR1 complex IIa and complex IIb depends on non-ubiquitylated RIPK1. For the formation of complex IIa, ubiquitylated RIPK1 in complex I is deubiquitylated by CYLD. This deubiquitylated RIPK1 dissociates from the membrane-bound complex and moves into the cytosol, where it interacts with TRADD, FADD, Pro-caspase 8 and FLIPL to form complex IIa. By contrast, complex IIb is formed when the RIPK1 in complex I is not ubiquitylated owing to conditions that have resulted in the depletion of cIAPs, which normally ubiquitylate RIPK1. This non-ubiquitylated RIPK1 dissociates from complex I, moves into the cytosol, and assembles with FADD, Pro-caspase 8, FLIPL and RIPK3 (but not TRADD) to form complex IIb. For either complex IIa or complex IIb to prevent necroptosis, both RIPK1 and RIPK3 must be inactivated by the cleavage activity of the Pro-caspase 8-FLIPL heterodimer or fully activated caspase 8. The Pro-caspase 8 homodimer generates active Caspase 8, which is released from complex IIa and complex IIb. This active Caspase 8 then carries out cleavage reactions to activate downstream executioner caspases and thus induce classical apoptosis. 

 

Formation of the complex IIc (necrosome) is initiated either by RIPK1 deubiquitylation mediated by CYLD or by RIPK1 non-ubiquitylation due to depletion of cIAPs, similar to complex IIa and complex IIb formation. RIPK1 recruits numerous RIPK3 molecules. They come together to form amyloid microfilaments called necrosomes. Activated RIPK3 phosphorylates and recruits MLKL, eventually leading to the formation of a supramolecular protein complex at the plasma membrane and necroptosis [1][2].

 

Reference:
[1]. Brenner D, et al. Regulation of tumour necrosis factor signalling: live or let die.Nat Rev Immunol. 2015 Jun;15(6):362-74. 
[2]. Conrad M, et al. Regulated necrosis: disease relevance and therapeutic opportunities.Nat Rev Drug Discov. 2016 May;15(5):348-66. 
 

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