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-N6580
    Ginsenoside Rg4
    		Inhibitor 99.94%
    Ginsenoside Rg4 is an orally active protopanaxatriol type ginsenoside. Ginsenoside Rg4 can activate PI3K, AKT and GSK-3β signaling. Ginsenoside Rg4 can inhibit ROS and inflammatory cytokine levels. Ginsenoside Rg4 can be used for the researches of inflammation, infection and metabolic disease, such as sepsis and lung inflammation.
    Ginsenoside Rg4
  • HY-P991402
    BI-1910
    		Inhibitor 98.24%
    BI-1910 is a human monoclonal antibody (mAb) targeting TNFRSF1B. BI-1910 enhances T cell activation and induces CD8 T cell-dependent anti-tumor effects. BI-1910 can be used in solid tumors research. Recommended isotype control: Human IgG2 lambda, Isotype Control (HY-P991206).
    BI-1910
  • HY-N7926S
    Pentadecane-d32
    		Inhibitor 99.2%
    Pentadecane-d32 is the deuterium labeled Pentadecane (HY-N7926). Pentadecane is an orally active natural plant volatile alkane with anti-inflammatory, analgesic, antipyretic and anti-leishmanial activities. Pentadecane presents IC50 values of 65.3 μM, 60.5 μM and 194.8 μM against Leishmania infantum promastigotes, amastigotes and intracellular amastigotes, respectively. Pentadecane downregulates the mRNA expression of TNF-α and IL-12 and inhibits the release of inflammatory mediators. Pentadecane arrests the cell cycle of Leishmania infantum and induces apoptosis. Pentadecane can be applied to the research of inflammation and leishmaniasis.
    Pentadecane-d<sub>32</sub>
  • HY-N2195R
    Nootkatone (Standard)
    		Inhibitor
    Nootkatone (Standard) is the analytical standard of Nootkatone. This product is intended for research and analytical applications. Nootkatone, a neuroprotective agent from Vitis vinifera, has antioxidant and anti-inflammatory effects[1]. Nootkatone improves cognitive impairment in lipopolysaccharide-induced mouse model of Alzheimer's disease[2].
    Nootkatone (Standard)
  • HY-P991063
    GEN-1053
    		Inhibitor 99.72%
    GEN-1053 (BNT-313) is a fully human IgG1 antibody that targets CD27. GEN-1053 binds to CD27 and forms a hexamer upon binding. The isotype control for GEN-1053 can refer to Human IgG1 lambda1, Isotype Control (HY-P99992).
    GEN-1053
  • HY-121309
    Doxorubicinone
    		Inhibitor 98.29%
    Doxorubicinone (Adriamycin aglycone) is the aglycone of the antibiotic Doxorubicin (HY-15142A), i.e., its sugar-free parent nucleus structure. Doxorubicinone does not induce DNA damage or bind to RelA, but still downregulates the expression of pro-inflammatory cytokines (such as TNF, IL-12, etc.) regulated by the NF-κB pathway. Doxorubicinone can be used in sepsis-related research.
    Doxorubicinone
  • HY-N10913
    Chloranthalactone B
    		Inhibitor
    Chloranthalactone B, a lindenane-type sesquiterpenoid, is a nature product that could be isolated from Chinese medicinal herb Sarcandra glabra. Chloranthalactone B inhibits the production of inflammatory mediators by inhibiting the AP-1 and p38 MAPK pathways.
    Chloranthalactone B
  • HY-179421
    PROTAC HDAC6 degrader 7
    		Inhibitor
    PROTAC HDAC6 degrader 7 is an orally active, highly efficient, and selective PROTAC degrader targeting histone deacetylase 6 (HDAC6) (IC50 = 118 nM). PROTAC HDAC6 degrader 7 can eliminate both the catalytic and zinc-finger ubiquitin-binding domain. PROTAC HDAC6 degrader 7 inhibits NLRP3 inflammasome assembly and activation, as well as blocks NF-κB signaling, thereby reducing the transcription and release of key inflammatory factors. PROTAC HDAC6 degrader 7 can reduce the mRNA levels of NLRP3, pro-IL-1β, TNF-α, and IL-6. PROTAC HDAC6 degrader 7 can be used for the study of inflammatory bowel disease (IBD).
    PROTAC HDAC6 degrader 7
  • HY-P990249
    Anti-Mouse DR5/CD262 Antibody (MD5-1)
    		Inhibitor 99.20%
    Anti-Mouse DR5/CD262 Antibody (MD5-1) is an anti-mouse DR5/CD262 IgG monoclonal antibody. Anti-Mouse DR5/CD262 Antibody (MD5-1) can eliminate myeloid derived suppressor cells (MDSCs) and enhance T cell anti-tumor immunity. Anti-Mouse DR5/CD262 Antibody (MD5-1) can be used for research on cancer such as gastric and colon cancer.
    Anti-Mouse DR5/CD262 Antibody (MD5-1)
  • HY-178037
    TLR9 antagonist 1
    		Inhibitor
    TLR9 antagonist 1 is a selective hTLR9 antagonist with an IC50 of 0.1 nM against hTLR9. TLR9 antagonist 1 exhibits favorable pharmacokinetic and pharmacodynamic properties. TLR9 antagonist 1 can be used in the research of systemic lupus erythematosus.
    TLR9 antagonist 1
  • HY-P990526
    Anti-TNFRSF21/DR6/CD358 Antibody
    		Inhibitor 98.58%
    Anti-TNFRSF21/DR6/CD358 Antibody is a CHO-expressed humanized antibody that targets TNFRSF21/DR6/CD358. The Anti-TNFRSF21/DR6/CD358 Antibody has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-TNFRSF21/DR6/CD358 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-TNFRSF21/DR6/CD358 Antibody
  • HY-P991439
    BIIB023
    		Inhibitor
    BIIB023 is a human monoclonal antibody (mAb) targeting TNFRSF12A/TWEAKR/CD266. BIIB023 can be used in lupus nephritis and rheumatoid arthritis research.
    BIIB023
  • HY-P991151
    Opamtistomig
    		Inhibitor
    Opamtistomig is a humanized immunoglobulin (H-γ1-scFv-L-κ) dimer monoclonal antibody targeting human programmed death ligand 1 (PD-L1), CD274 and tumor necrosis factor receptor superfamily member 9 (TNFRSF9). Opamtistomig is promising for research of various solid tumors and hematological malignancies.
    Opamtistomig
  • HY-147086
    CAY10789
    		Inhibitor 99.84%
    CAY10789 is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases.
    CAY10789
  • HY-100376
    CPI-1189
    		Inhibitor 99.82%
    CPI-1189 is an orally active TNF-α release inhibitor. CPI-1189 inhibits phosphorylation of p38. CPI-1189 can inhibit apoptosis. CPI-1189 can be used in the study of HIV and neurological diseases.
    CPI-1189
  • HY-P991682
    Emzotamig
    		Inhibitor
    Emzotamig is a monoclonal antibody inhibitor targeting tumor necrosis factor (TNF). Emzotamig is promising for research of autoimmune diseases associated with TNF overexpression, such as rheumatoid arthritis and ankylosing spondylitis.
    Emzotamig
  • HY-P992101
    Aritinercept
    		Inhibitor 99.90%
    Aritinercept (AUR-200) is a recombinant fusion protein targeting TNFSF13B/BAFF/CD257. Aritinercept neutralizes BAFF and APRIL (TNFSF13), reduces B cell proliferation, suppresses peripheral B cells, lowers serum immunoglobulins. Aritinercept reduces renal damage markers, decreases IFNγ, IL-17A, and anti-dsDNA autoantibodies, and improves survival in a mouse model of SLE. ritinercept can be used for the research of systemic lupus erythematosus.
    Aritinercept
  • HY-172774
    TRPV1 antagonist 10
    		Inhibitor 98.54%
    TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC50 = 33.06 nM), moderate to weak URAT1 (IC50 = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain.
    TRPV1 antagonist 10
  • HY-N0509R
    Astilbin (Standard)
    		Inhibitor
    Astilbin (Standard) is the analytical standard of Astilbin. This product is intended for research and analytical applications. Astilbin is a flavonoid compound and enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.
    Astilbin (Standard)
  • HY-148552
    Anti-inflammatory agent 35
    		Inhibitor 99.77%
    Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue with anti-inflammatory activity. Anti-inflammatory agent 35 blocks mitogen-activated protein kinase (MAPK) signaling and p65 nuclear translocation of NF-kB. Anti-inflammatory agent 35 also inhibits yellow neutrophil infiltration and pro-inflammatory cytokine production. Anti-inflammatory agent 35 significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI) in vivo.
    Anti-inflammatory agent 35
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. 
 

TNF Receptor Isoform Comparison

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