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-N5054
    (R)-5,7-Dimethoxyflavanone
    Inhibitor ≥99.0%
    (R)-5,7-Dimethoxyflavanone shows potent antimutagenic activity against MeIQ mutagenesis in Ames test using the S. typhimurium TA100 and TA98 strains. And (R)-5,7-Dimethoxyflavanone significantly and dose-dependently inhibits the inflammatory mediato.
    (R)-5,7-Dimethoxyflavanone
  • HY-P990269
    Anti-Mouse CD40L/CD154 (LALA-PG) Antibody (MR-1)
    Inhibitor
    Anti-Mouse CD40L/CD154 (LALA-PG) Antibody (MR-1) is a mouse-derived IgG2a, κ type antibody inhibitor, targeting to mouse CD40L/CD154.
    Anti-Mouse CD40L/CD154 (LALA-PG) Antibody (MR-1)
  • HY-P990742
    Givastomig
    Givastomig is an anti-TNFRSF9/CLDN18 monoclonal antibody.
    Givastomig
  • HY-113763
    TWEAK-Fn14-IN-1
    TWEAK-Fn14-IN-1 (Compound L524-0366) is a specific dose-dependent TWEAK-Fn14 inhibitor. TWEAK-Fn14-IN-1 binds specifically to the Fn14 surface with a KD of 7.12 μM. TWEAK-Fn14-IN-1 inhibits TWEAK induced glioma cell migration without any potential cytotoxic effects.
    TWEAK-Fn14-IN-1
  • HY-N0724R
    Mesaconitine (Standard)
    Inhibitor
    Mesaconitine (Standard) is the analytical standard of Mesaconitine. This product is intended for research and analytical applications.
    Mesaconitine (Standard)
  • HY-N6927R
    Isoforskolin (Standard)
    Inhibitor
    Isoforskolin (Standard) is the analytical standard of Isoforskolin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-161833
    HSP90-IN-31
    Inhibitor
    HSP90-IN-31 (compound Be01) causes reduction of CD80 and CD86 expression on dendritic cells (DCs). HSP90-IN-31 decreases the production of pro-inflammatory cytokines (IL-6, TNF-α, and IL-1β) in BMDC and peritoneal macrophages stimulated by LPS (HY-D1056). Under the delayed-type hypersensitivity (DTH) mice model, HSP90-IN-31 reduces ear swelling and pro-inflammatory cytokines in the spleen.
    HSP90-IN-31
  • HY-N0042R
    Ginsenoside Rc (Standard)
    Inhibitor
    Ginsenoside Rc (Standard) is the analytical standard of Ginsenoside Rc. This product is intended for research and analytical applications. Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
    Ginsenoside Rc (Standard)
  • HY-P99543
    Tulinercept
    Inhibitor
    Tulinercept (OPRX-106) is a recombinant TNF receptor fusion protein fused to an IgG1 Fc domain.
    Tulinercept
  • 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
    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-115351
    GW-3333
    Inhibitor
    GW-3333 is a potent and orally active TNF-alpha-converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitor. GW-3333 inhibits tumor necrosis factor-alpha (TNF-alpha) production. GW-3333 can be used in research of arthritis.
    GW-3333
  • HY-N2350R
    Cynaropicrin (Standard)
    Inhibitor
    Cynaropicrin (Standard) is the analytical standard of Cynaropicrin. This product is intended for research and analytical applications. Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
    Cynaropicrin (Standard)
  • HY-N8903
    Mumefural
    Inhibitor
    Mumefural is a bioactive component of the processed fruit of Prunus mume Sieb. Mumefural inhibits platelet aggregation. Mumefural shows anti-thrombotic effects and ameliorates cognitive impairment.
    Mumefural
  • HY-161381
    PDE4-IN-15
    Inhibitor
    PDE4-IN-15 (compound 7b-1) is an inhibitor of PDE4 (IC50 = 0.17 μM) and has anti-TNF-α activity (EC50 = 0.19 μM). PDE4-IN-15 has a good skin permeability.
    PDE4-IN-15
  • HY-146547
    Anti-inflammatory agent 17
    Inhibitor
    Anti-inflammatory agent 17 is a potent and orally active anti-inflammatory agent. Anti-inflammatory agent 17 inhibits the release of IL-6 and TNF-α in vitro experiments without cytotoxicity. Anti-inflammatory agent 17 exhibits anti-inflammatory activity in vivo. Anti-inflammatory agent 17 has the potential for the research of Acute lung injury (ALI).
    Anti-inflammatory agent 17
  • HY-19570A
    NSC 15830 hydrochloride
    Inhibitor
    NSC 15830 (S-(1,2-Dichlorovinyl)-L-cysteine) hydrochloride is a nephrotoxin and metabolite of trichloroethylene. NSC 15830 hydrochloride inhibits pathogen-stimulated TNF-α.
    NSC 15830 hydrochloride
  • HY-B0026R
    Ceftiofur hydrochloride (Standard)
    Inhibitor
    Ceftiofur hydrochloride (Standard) is the analytical standard of Ceftiofur hydrochloride (HY-B0026). This product is intended for research and analytical applications. Ceftiofur hydrochloride is a cell wall synthesis inhibitor that targets bacterial penicillin-binding proteins (PBPs) and has anti-inflammatory effects in endotoxemia. Ceftiofur hydrochloride exerts bactericidal effects by inhibiting the synthesis of bacterial cell wall peptidoglycan, leading to bacterial cell lysis. Ceftiofur hydrochloride also inhibits the activation of NF-κB and MAPKs, thereby reducing the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6.
    Ceftiofur hydrochloride (Standard)
  • HY-173334
    hMAO-B-IN-11
    Inhibitor
    hMAO-B-IN-11 (Compound 12) is a selective and reversible inhibitor of human monoamine oxidase B (hMAO-B) with an IC50 of 0.11 µM. hMAO-B-IN-11 acts through competitive binding to the hMAO-B active site, preventing oxidative deamination of monoamines and reducing hydrogen peroxide production. hMAO-B-IN-11 also inhibits pro-inflammatory mediators (NO, TNF-α, IL-1β) in activated microglia, hMAO-B-IN-11 is promising for research of neurodegenerative diseases like Parkinson’s and Alzheimer’s.
    hMAO-B-IN-11
  • HY-160027
    TNF-alpha-IN-1
    Inhibitor
    TNF-alpha-IN-1 (compound 202) is an orally active inhibitor of TNF-alpha. TNF-alpha-IN-1 has anti-inflammatory activity which can used in study rheumatoid arthritis, psoriasis, and asthma.
    TNF-alpha-IN-1
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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