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-W011404R
    Tributyrin (Standard)
    Inhibitor
    Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed proagent of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects.
    Tributyrin (Standard)
  • HY-182006
    TNF-α-IN-28
    Inhibitor
    TNF-α-IN-28 (compound 4ea) is a TNF-α and NF-κB inhibitor with anti-inflammatory activity. TNF-α-IN-28 inhibits TNF-α and NF-κB expression. TNF-α-IN-28 interacts with TNF-α dimer.
    TNF-α-IN-28
  • 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-P10994
    Eps8 peptide 327
    Inhibitor
    Eps8 peptide 327 is an HLA-A*2402-restricted peptide antigen derived from Eps8 protein. Eps8 peptide 327 has potent antitumor activity with significant cytotoxicity. Eps8 peptide 327 effectively inhibits cancer cells proliferation, induces apoptosis and disrupts EGFR signal pathway by inhibiting downstream signals (such as IL-2, TNF-α and IFN-γ) expression and the Eps8/EGFR interaction. Eps8 peptide 327 significantly inhibits tumor growth in HT-29 xenograft mcie models.
    Eps8 peptide 327
  • 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-P991362
    GB-223
    Inhibitor
    GB-223 is a human monoclonal antibody (mAb) targeting TNFSF11/RANKL/CD254. GB-223 can be used in Giant cell tumour of bone and Postmenopausal osteoporosis research.
    GB-223
  • 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-N17395
    (6R,7R)-Epoxy-1-oleanen-3-ol
    Inhibitor
    (6R,7R)-Epoxy-1-oleanen-3-ol is a triterpenoid that can be found in Boswellia ovalifoliolata, exhibiting anti-inflammatory activity. (6R,7R)-Epoxy-1-oleanen-3-ol inhibits TNF-α, IL-6, IL-8, and NO production in LPS (HY-D1056)-activated murine neutrophils. (6R,7R)-Epoxy-1-oleanen-3-ol can be used for the research on inflammatory conditions.
    (6R,7R)-Epoxy-1-oleanen-3-ol
  • 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-N15589
    8-(6,7-Dihydroxy-3,7-dimethyl-2E-octenyloxy)psoralen
    Inhibitor
    8-(6,7-Dihydroxy-3,7-dimethyl-2E-octenyloxy)psoralen is a compound found in Citrus grandis. 8-(6,7-Dihydroxy-3,7-dimethyl-2E-octenyloxy)psoralen has significant anti-inflammatory activity, which mainly works by inhibiting the secretion of inflammatory factors IL-1β, PGE2 and TNF-α. 8-(6,7-Dihydroxy-3,7-dimethyl-2E-octenyloxy)psoralen can be used in the study of inflammation.
    8-(6,7-Dihydroxy-3,7-dimethyl-2E-octenyloxy)psoralen
  • 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
  • HY-108162A
    Ataquimast
    Inhibitor
    Ataquimast is a COX-2 inhibitor that inhibits the release of leukotrienes, TNF-α and GM-CSF. Ataquimast can be used in the study of advanced receptor-positive breast cancer.
    Ataquimast
  • HY-P11098
    Peptide HV2
    Inhibitor
    Peptide HV2 is an antibiotic that exerts anti-inflammatory effects by inhibiting TNF-α. Peptide HV2 has antibacterial activity.
    Peptide HV2
  • HY-P991465
    Anti-CD27 Antibody (M2177)
    Inhibitor
    Anti-CD27 Antibody (M2177) is a human monoclonal antibody (mAb) targeting TNFRSF7/CD27. Anti-CD27 Antibody (M2177) inhibits the binding of sCD70 to human CD27 ECD-Fc. Anti-CD27 Antibody (M2177) can be used in the study of anti-tumor immunity. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-CD27 Antibody (M2177)
  • HY-130054
    Theophylline L-lysine
    Inhibitor
    Theophylline L-lysine (Lysine theophyllinate) is a soluble derivative of Theophylline (HY-B0809). Theophylline L-lysine is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline L-lysine inhibits PDE3 activity to relax airway smooth muscle. Theophylline L-lysine has anti-inflammatory activity by increasing IL-10 and inhibiting NF-κB into the nucleus. Theophylline L-lysine induces apoptosis. Theophylline L-lysine can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline L-lysine
  • HY-182630
    CJ-14897
    Inhibitor
    CJ-14897 is a cytokine production inhibitor, with IC50 values of 0.059 μM and 0.59 μM for IL-1β and TNF-α production, respectively, and an IC50 of 180 μM for leucine uptake. CJ-14897 is isolated from the fermentation broth of the basidiomycete Marasmius strain CL21624.
    CJ-14897
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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