2. Signaling Pathways
  3. Apoptosis
  4. TNF Receptor

TNF Receptor

Tumor Necrosis Factor Receptor; TNFR

TNF Receptor

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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.

TNF Receptor Isoform Specific Products:

TNF Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N0528R
    Linarin (Standard)
    Linarin (Standard) is the analytical standard of Linarin. This product is intended for research and analytical applications. Linarin (Buddleoside) is an orally active and selective inhibitor of acetylcholinesterase (AChE). Linarin has many activities, such as anti-inflammatory, antioxidant, sleep aid and sedation, bone differentiation, anti-tumor, antibacterial and antiviral. Linarin can be used to study diseases such as the nervous system, osteoporosis and cancer.
    Linarin (Standard)
  • HY-W040045R
    Callistephin chloride (Standard)
    		Inhibitor
    Callistephin (Pelargonidin 3-O-glucoside) chloride (Standard) is the analytical standard of Callistephin chloride (HY-W040045). This product is intended for research and analytical applications. Callistephin chloride is an anthocyanin. Callistephin chloride regulates the expression of inflammatory (reducing iNOS/TNF-α/COX-2) and apoptosis-related proteins by inhibiting p38 phosphorylation, and enhances the protective effect of Isoflurane (HY-A0134) on microglial cell damage. Callistephin chloride significantly reduces ROS levels, eliminates DPPH free radicals, protects retinal pigment epithelial cells, and inhibits lipid peroxidation. Callistephin chloride can alleviate glutamate excitotoxicity, reduce neuronal apoptosis, and protect cerebellar granule neurons. Callistephin chloride can inhibit the proliferation and metastasis of breast cancer cells by inducing apoptosis.
    Callistephin chloride (Standard)
  • HY-P990528
    Anti-TNFRSF7/CD27 Antibody
    		Inhibitor
    Anti-TNFRSF7/CD27 Antibody is a CHO-expressed human antibody targeting TNFRSF7/CD27. The Anti-TNFRSF7/CD27 Antibody contains huIgG2 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Anti-TNFRSF7/CD27 Antibody can refer to Human IgG2 kappa, Isotype Control (HY-P99002).
    Anti-TNFRSF7/CD27 Antibody
  • HY-106359
    Delmitide
    		Inhibitor
    Delmitide (RDP58) is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide can be used for the research of ulcerative colitis.
    Delmitide
  • HY-N15651
    Asperflavin
    		Inhibitor
    Asperflavin is an anti-inflammatory compound that can be produced by the marine fungus Eurotium amstelodami. Asperflavin inhibits the production of NO, PGE2, and proinflammatory cytokines, as well as the expression of inducible NOS (iNOS) in RAW 264.7 cells treated with LPS (HY-D1056). Asperflavin can be used in the study of inflammatory diseases.
    Asperflavin
  • HY-P991634
    IBI-325
    		Inhibitor
    IBI-325 is a humanized monoclonal antibody inhibitor targeting CD73. IBI-325 completely inhibits CD73 enzymatic activity without hook effect. IBI-325 reverses Adenosine monophosphate (HY-A0181)-mediated immune suppression and significantly inhibits T cell proliferation and cytokines (IL-2, IFN-γ and TNF-α) release. IBI-325 has potent antitumor activities in hPBMC-reconstituted mice model and hCD73 knock-in mice model. IBI-325 can be used for cancer immunotherapy research.
    IBI-325
  • HY-122566
    SMU127
    		Inducer
    SMU127 is an agonist of the toll-like receptor 1/2 (TLR1/2) heterodimer. It induces NF-κB signaling in cells expressing human TLR2 (EC50=0.55 μM) but not cells expressing human TLR3, -4, -5, -7, or -8 when used at concentrations ranging from 0.1 to 100 μM. SMU127 induces the production of TNF-α in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 0.01 to 1 μM. In vivo, SMU127 (0.1 mg/animal) reduces tumor volume in a 4T1 murine mammary carcinoma model.
    SMU127
  • HY-173180
    5-LOX-IN-8
    		Inhibitor
    5-LOX-IN-8 is a 5-LOX inhibitor with anti-inflammatory activity. 5-LOX-IN-8 suppresses IL-6, IL-1β, TNF-α and IFN-γ in macrophages and reduces IL-8 secretion in SW480 cells. 5-LOX-IN-8 reduces disease activity in a DSS colitis model. 5-LOX-IN-8 can be used for research of inflammatory bowel disease (IBD).
    5-LOX-IN-8
  • HY-B0809B
    Theophylline sodium acetate
    		Inhibitor
    Theophylline (1,3-Dimethylxanthine) sodium acetate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) sodium acetate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) sodium acetate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) sodium acetate induces apoptosis. Theophylline (1,3-Dimethylxanthine) sodium acetate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline sodium acetate
  • HY-173210
    TNF-α-IN-22
    		Inhibitor
    TNF-α-IN-22 (Compound 30) is a TNFα inhibitor. It can induce Apoptosis by inhibiting the downregulation of IkBα induced by TNFα and blocking the cell cycle. TNF-α-IN-22 can be used in the research of triple-negative breast cancer.
    TNF-α-IN-22
  • HY-N6739R
    Beauvericin (Standard)
    Doxycycline (monohydrate) (Standard) is the analytical standard of Doxycycline (monohydrate). This product is intended for research and analytical applications. Doxycycline monohydrate is an antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor.
    Beauvericin (Standard)
  • HY-160436
    TNF-α-IN-15
    		Inhibitor
    TNF-α-IN-15 is a TNF-α inhibitor. TNF-α-IN-15 can decrease the TNF-α blood levels.
    TNF-α-IN-15
  • HY-P990980
    Cizutamig
    		Inhibitor
    HY-P990980 is an TNFRSF17-targeting [L-κ-H-γ1_[VH-G1(CH1-h)]_Lκ] dimer type humanized antibody.
    Cizutamig
  • HY-P991432
    VTX-0811
    		Activator
    VTX-0811 is a human IgG4 monoclonal antibody (mAb) targeting PSGL1/CD162. VTX-0811 up-regulates TNF-α/NF-κB and chemokine-mediated signaling and down-regulates oxidative phosphorylation, fatty acid metabolism, and Myc signaling pathways. VTX-0811 increases the proportion of CD8+ T cells among infiltrating T cells. VTX-0811 has antitumor activity in a humanized mouse PDX model of melanoma.
    VTX-0811
  • HY-125740R
    Malvidin-3-glucoside chloride (Standard)
    		Inhibitor
    Malvidin-3-glucoside (Malvidin-3-O-glucoside; Oenin) chloride (Standard) is the analytical standard of Malvidin-3-glucoside chloride (HY-125740). This product is intended for research and analytical applications. Malvidin-3-glucoside chloride is an orally active inhibitor of the NF-κB pathway, which blocks inflammatory responses induced by TNF-α, reduces IκB-α degradation and p65 nuclear translocation, and upregulates endothelial nitric oxide synthase eNOS to increase NO production. Malvidin-3-glucoside chloride exerts anti-inflammatory and antioxidant effects by inhibiting pro-inflammatory molecules such as MCP-1, ICAM-1, and IL-6, and regulating intestinal microorganisms and metabolites, while protecting endothelial cells and improving intestinal microecological dysbiosis under inflammatory conditions. Malvidin-3-glucoside chloride can be used to study chronic inflammatory-related diseases such as atherosclerosis and inflammatory bowel disease, and has the potential to prevent vascular inflammation and improve intestinal health.
    Malvidin-3-glucoside chloride (Standard)
  • HY-N9867
    Gnetifolin E
    		Inhibitor
    Gnetifolin E is a resveratrol trimer derivative that can be isolated from Gnetum brunonianum. Gnetifolin E has anti-inflammatory activity, and inhibits TNF-α.
    Gnetifolin E
  • HY-Y0399S
    L-Norvaline-d5
    		Antagonist
    L-Norvaline-d5 is the deuterium labeled L-Norvaline. L-Norvaline is the inhibitor for arginase, that promotes the production of NO, reduces oxidative stress, improves insulin resistance, and exhibits antioxidant and anti-hyperglycemic effects. L-Norvaline can be used in research of Alzheimer’s disease.
    L-Norvaline-d<sub>5</sub>
  • HY-177305
    Anti-inflammatory agent 105
    		Inhibitor
    Anti-inflammatory agent 105 (Compound 12) is an anti-inflammatory compound. The IC50 of Anti-inflammatory agent 105 for the inhibition of TNF-α synthesis and release in the human macrophage cell line U937 is 0.124 nM.
    Anti-inflammatory agent 105
  • HY-P990304C
    Anti-Mouse 4-1BBL/CD137L (LALA-PG) Antibody (TKS-1)
    		Inhibitor
    Anti-Mouse 4-1BBL/CD137L (LALA-PG) Antibody (TKS-1) is a mouse-derived IgG2a κ antibody inhibitor that targets mouse 4-1BBL/CD137L.Anti-Mouse 4-1BBL/CD137L (LALA-PG) Antibody (TKS-1) is a chimeric version of the original TKS-1 antibody (HY-P990304). The variable domain sequences are identical to the original TKS-1 but the constant region sequences have been switched from rat IgG2a to mouse IgG2a. Anti-Mouse 4-1BBL/CD137L (LALA-PG) Antibody (TKS-1) contains a LALA-PG mutation in the Fc fragment rendering it unable to bind to endogenous Fcγ receptors. Anti-Mouse 4-1BBL/CD137L (LALA-PG) Antibody (TKS-1) reacts with mouse 4-1BB ligand (4-1BBL). Anti-Mouse 4-1BBL/CD137L (LALA-PG) Antibody (TKS-1) can be used for the researches of cancer, infection, inflammation and immunology.
    Anti-Mouse 4-1BBL/CD137L (LALA-PG) Antibody (TKS-1)
  • HY-153329
    TNF-α-IN-9
    		Inhibitor
    TNF-α-IN-9 (compound 48) is a analog of NDM-1 inhibitor-3 (HY-150758). TNF-α-IN-9 is a TNF-α inhibitor. TNF-α-IN-9 shows low inhibitory activity.
    TNF-α-IN-9
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
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Download TNF Receptor Signaling Pathway Map.

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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