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-182308
    LC-PDA-01
    		Inhibitor
    LC-PDA-01 is a selective peroxiredoxin 1 (PRDX1) activator with an EC50 of 111.8 nM and a human KD of 123.2 nM. LC-PDA-01 inhibits the expression of pro-inflammatory cytokines IL-1β, IL-6 and TNF-α. LC-PDA-01 can be used in antioxidant/anti-inflammatory research.
    LC-PDA-01
  • HY-P991557
    ABI793
    		Inhibitor
    ABI793 is a human IgG1 anti-human CD154 (CD40 ligand) monoclonal antibody. ABI793 inhibits immune response by blocking the CD154-CD40 (IC50 = 75 nM) signaling pathway. ABI793 effectively prevents kidney transplant rejection. ABI793 can be used for research on immunological rejection.
    ABI793
  • HY-183611
    LPZ-51
    		Inhibitor
    LPZ-51 is a Vibrio β-lactam resistance sensor kinase (VbrK) inhibitor with a Ki value of 1.09 μM. LPZ-51 inhibits blaA gene expression at the transcriptional level by blocking the kinase activity of VbrK, reduces β-lactamase synthesis, and does not affect bacterial growth. LPZ-51 acts synergistically with β-lactam antibiotics. LPZ-51 decreases bacterial load, alleviates intestinal inflammation, and improves survival rate in zebrafish infection models. LPZ-51 can be used in studies related to Vibrio parahaemolyticus infection.
    LPZ-51
  • HY-P992354
    FPA154
    		Inhibitor
    FPA154 is a human monoclonal antibody against TNFRSF18/GITR/CD357. FPA154 activates NF-κB via the GITR pathway. FPA154 can be used in solid tumor research. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
    FPA154
  • HY-P991408
    DLX-105
    		Inhibitor
    DLX-105 is a human monoclonal antibody (mAb) targeting TNFSF2/TNFa. DLX-105 reduces skin epidermal thickness and the expression of K16 and Ki67. DLX-105 down-regulates the mRNA levels of IL-17, TNF-α, IL-23p19, IL-12p40, and IFN-γ. DLX-105 can be used in psoriasis research.
    DLX-105
  • HY-105488
    MDL 201112
    		Inhibitor
    MDL 201112 is a carbocyclic nucleoside. MDL 201112 can decrease TNF-α production and inhibit MHC class II Ia+ antigen expression. MDL 201112 can be used for the research of inflammation and immunology.
    MDL 201112
  • HY-P991409
    GSK2800528
    		Inhibitor
    GSK2800528 is a human monoclonal antibody (mAb) targeting TNFSF2/TNFa. GSK2800528 can be used in inflammation and psoriasis research.
    GSK2800528
  • HY-171468
    CC-1069
    		Inhibitor
    CC-1069, a structural analog of thalidomide (HY-14658), is a TNF-α inhibitor that inhibits endothelial. CC-1069 can be used to study angiogenesis-dependent tumors such as gliomas.
    CC-1069
  • HY-P991473
    hCBE-11
    		Inhibitor
    hCBE-11 is a human monoclonal antibody (mAb) targeting TNFRSF3. hCBE-11 can be used in solid tumors research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).
    hCBE-11
  • HY-181156
    Anti-inflammatory agent 112
    		Inhibitor
    Anti-inflammatory agent 112 is an inducible nitric oxide synthase (iNOS) inhibitor, a COX-2 inhibitor, and an anti-inflammatory agent. Anti-inflammatory agent 112 suppresses i-NOS and COX-2 protein expression, reduces nitric oxide, IL-6, and TNF-α production, and attenuates lipopolysaccharide (LPS)-induced inflammatory responses. Anti-inflammatory agent 112 can be used for the research of inflammatory disorders.
    Anti-inflammatory agent 112
  • 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-182884
    TNF-α-IN-29
    		Inhibitor
    TNF-α-IN-29 is an orally active and selective TNF-α inhibitor, with IC50 values of 123.0 nM against human targets, and a human Kd of 45.9 nM. TNF-α-IN-29 blocks TNF-α-TNFR1 protein-protein interactions and inhibits TNF-α-mediated inflammatory signaling pathways. TNF-α-IN-29 exhibits anti-inflammatory effects in a mouse model of collagen-induced arthritis and promotes articular cartilage repair. TNF-α-IN-29 can be used for the research of rheumatoid arthritis.
    TNF-α-IN-29
  • 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-N17773
    Hydrangeic acid
    		Inhibitor
    Hydrangeic acid is an orally effective stilbene-type glycolipid metabolism regulator that lowers blood glucose and lipids. It can be isolated from processed leaves of Hydrangea macrophylla var. thunbergii. Hydrangeic acid is associated with glycolipid metabolism and insulin sensitivity regulation. Hydrangeic acid does not directly activate PPARγ or PPARα, but instead upregulates the mRNA expression of adiponectin, PPARγ2, GLUT4, and fatty acid-binding protein aP2, and downregulates TNF-α mRNA expression, promoting adipogenesis, glucose uptake, and GLUT4 translocation in 3T3-L1 cells. Simultaneously, Hydrangeic acid inhibits inflammatory factor-induced NO production, exerting activity in improving insulin resistance. Hydrangeic acid can be used in research related to type 2 diabetes and does not cause liver weight gain as a side effect.
    Hydrangeic acid
  • 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-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
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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