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-145726A
    ISIS 104838 sodium
    ISIS 104838 sodium is an antisense oligonucleotide agent that reduces the production of tumor necrosis factor (TNF-alpha), a substance that contributes to joint pain and swelling in rheumatoid arthritis.
    ISIS 104838 sodium
  • HY-145498
    HDMAPP triammonium
    Activator
    HDMAPP triammonium is a potent phosphoantigen in the ammonium form and the pyrophosphate form of (E)-HDMAPP. HDMAPP is also a potent activator of γδ T cells and can induce T cell stimulation in vitro (EC50=0.39 nM, TNF-α).
    HDMAPP triammonium
  • HY-P99940
    Remtolumab
    Inhibitor 99.24%
    Remtolumab (ABT-122) is a dual-variable domain immunoglobulin that neutralises both tumor necrosis factor α (TNFα) and IL-17A. Remtolumab shows dual inhibition of TNFα and IL-17A. Remtolumab can be used for rheumatoid arthritis (RA) research.
    Remtolumab
  • HY-P990715
    Ozekibart
    99.63%
    Ozekibart is an anti-TNFRSF10B monoclonal antibody.
    Ozekibart
  • HY-P2612
    WP9QY
    Antagonist 99.78%
    WP9QY, TNF-a Antagonist, TNF-a Antagonist is a biological active peptide. (This cyclic peptide is designed to mimic the most critical tumor necrosis factor (TNF) recognition loop on TNF receptor I. It prevents interactions of TNF with its receptor. This TNF antagonist is a useful template for the development of small molecular inhibitors to prevent both inflammatory bone destruction and systemic bone loss in rheumatoid arthritis.)
    WP9QY
  • HY-P1825A
    TNF-α (10-36), human TFA
    TNF-α (10-36), human (TFA) is a peptide of human TNF-α.
    TNF-α (10-36), human TFA
  • HY-126818
    Desfuroylceftiofur
    Inhibitor
    Desfuroylceftiofur is an active metabolite of Ceftiofur which is a broad-spectrum cephalosporin antibiotic. Desfuroylceftiofur is active against gram-positive and gram-negative bacteria.
    Desfuroylceftiofur
  • HY-133807A
    (Rac)-Benpyrine
    Inhibitor 99.30%
    (Rac)-Benpyrine, a racemate of Benpyrine, is a potent and orally active TNF-α inhibitor. (Rac)-Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
    (Rac)-Benpyrine
  • HY-P990726
    Abiprubart
    99.00%
    Abiprubart is an anti-CD40 human IgG4 κ monoclonal antibody. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).
    Abiprubart
  • HY-P99701
    Letolizumab
    Inhibitor
    Letolizumab (BMS-986004) is a monoclonal antibody targeting CD40L, which is produced to express mutant IgG1 lacking effector function, including Fc binding and complement fixation. Letolizumab reduces rejection, thromboembolism and prolongs the survival time.
    Letolizumab
  • HY-P1875
    TNF-α (46-65), human
    98.68%
    TNF-α (46-65), human is a peptide of TNF-α.
    TNF-α (46-65), human
  • HY-106359A
    Delmitide acetate
    Inhibitor 98.55%
    Delmitide (RDP58) acetate is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide acetate inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide acetate can be used for the research of ulcerative colitis.
    Delmitide acetate
  • HY-N6927
    Isoforskolin
    Inhibitor ≥98.0%
    Isoforskolin is the principle active component of C. forskohlii native to China. Isoforskolin reduces the secretion of lipopolysaccharide (LPS)-induced cytokines, namely TNF-α, IL-1β, IL-6 and IL-8, in human mononuclear leukocytes. Isoforskolin acts as an anti-inflammatory agent for the treatment of Lyme arthritis.
    Isoforskolin
  • HY-147078
    EJMC-1
    Inhibitor 99.69%
    EJMC-1 is a moderately potent TNF-α inhibitor with an IC50 value of 42 μM.
    EJMC-1
  • HY-N8593
    Undecane
    Inhibitor 99.66%
    Undecane has anti-allergic and anti-inflammatory activities on sensitized rat basophilic leukemia (RBL-2H3) mast cells and HaCaT keratinocytes. In sensitized mast cells, Undecane inhibits degranulation and the secretion of histamine and TNF-α[
    Undecane
  • HY-114095
    BML-280
    Inhibitor 99.64%
    BML-280 (VU0285655-1) is a potent and selective phospholipase D2 (PLD2) inhibitor. BML-280 has the ability to prevent caspase-3 cleavage and reduction in cell viability induced by high glucose. BML-280 can be used for rheumatoid arthritis research.
    BML-280
  • HY-N8277
    Kdo2-Lipid A ammonium
    Inducer 99.00%
    Kdo2-Lipid A ammonium is a chemically defined lipopolysaccharide (LPS) with endotoxin activity equal to LPS. Kdo2-Lipid A ammonium is highly selective for TLR4. Kdo2-Lipid A ammonium stimulates the release of both TNF and PGE2.
    Kdo2-Lipid A ammonium
  • HY-P2663
    Acetyl tetrapeptide-2
    99.70%
    Acetyl tetrapeptide-2 is a bioactive peptide with anti-aging effect and has been reported used as a cosmetic ingredient.
    Acetyl tetrapeptide-2
  • HY-P99663
    Inezetamab
    Inhibitor 99.77%
    Inezetamab is a bispecific anti-CD40 and anti-MSLN IgG1 monoclonal antibody.
    Inezetamab
  • HY-P991049
    Atrosimab
    Inhibitor 98.00%
    Atrosimab (ATM-001) is a Fv-Fc1κ fusion protein with strong binding to human TNFR1 with an EC50 value of 0.37 nM. Atrosimab potently inhibits TNF-induced activation of TNFR1. Atrosimab has the potential for the study of chronic inflammatory diseases.
    Atrosimab
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. 
 

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.