1. Signaling Pathways
  2. Apoptosis
  3. TNF Receptor

TNF Receptor

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-P99057
    Varlilumab
    Inhibitor
    Varlilumab (CDX-1127) is a first-in-class human IgG1 anti-CD27 monoclonal antibody. Varlilumab has an anti-tumor activity.
    Varlilumab
  • HY-N0152
    Myricitrin
    Inhibitor 99.64%
    Myricitrin, a naturally occurring flavonoid, is an orally active nitric oxide (NO) and PKC inhibitor. Myricitrin has central nervous system activity, including anxiolytic-like action. Myricitrin possesses antioxidant, anti-inflammatory, antifibrotic and anti-malarial effects.
    Myricitrin
  • HY-N0212
    Peimine
    Inhibitor 99.43%
    Peimine (Verticine; Dihydroisoimperialine) is an orally active natural product. Peimine has anti-inflammatory, analgesic and cough relieving effects. Peimine can be used in cancer and inflammation related research.
    Peimine
  • HY-111255A
    SPD304 dihydrochloride
    Inhibitor 99.96%
    SPD304 dihydrochloride is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 μM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.
    SPD304 dihydrochloride
  • HY-N0512
    Loganin
    Inhibitor 99.82%
    Loganin is a type of iridoid glycoside compound that possesses anti-inflammatory, antioxidant, and antitumor properties, and offers protective effects against acute lung injury and pulmonary fibrosis. Loganin exerts its protective effects against LPS (HY-D1056)-mediated inflammation and oxidative stress by upregulating the Nrf2/HO-1 signaling pathway, and it reduces neuroinflammation caused by spinal cord injury (SCI).
    Loganin
  • HY-P99446
    Atacicept
    Inhibitor 99.5%
    Atacicept (TACI-Ig) is a is a recombinant fusion protein containing the extracellular, ligand-binding portion of the TACI receptor and the Fc portion of human IgG. Atacicept inhibits B cell stimulation by binding to B lymphocyte stimulator and a proliferation-inducing ligand. Atacicept can be used in research of B-cell autoimmune disease.
    Atacicept
  • HY-P99049
    Sotigalimab
    Agonist 98.90%
    Sotigalimab, a CD40 agonistic monoclonal antibody. Sotigalimab binds CD40 with high affinity and activates antigen-presenting cells, thereby stimulating cancer-specific T cell responses. Sotigalimab is mainly used in the study of metastatic pancreatic cancer and metastatic melanoma.
    Sotigalimab
  • HY-124750
    NecroX-7
    Inhibitor 99.69%
    NecroX-7 is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor. NecroX-7 can be used as an antidote to acetaminophen toxicity. NecroX-7 exerts a protective effect by preventing the release of HMGB1 in ischemia/reperfusion injury. NecroX-7 inhibits the HMGB1-induced release of TNF and IL-6, as well as the expression of TLR-4 and receptor for advanced glycation end products. NecroX-7 can be used graft-versus-host disease (GVHD) research.
    NecroX-7
  • HY-N0267
    Hypaconitine
    Inhibitor 99.49%
    Hypaconitine, an active and highly toxic constituent derived from Aconitum species, is widely used to treat rheumatism.
    Hypaconitine
  • HY-Y0148
    10-Hydroxydecanoic acid
    Inhibitor 98.77%
    10-Hydroxydecanoic acid (10-HDAA) is a saturated fatty acid derived from 10-hydroxy-trans-2-decenoic acid, which can be isolated from royal jelly. 10-Hydroxydecanoic acid exhibits various biological activities, including anti-inflammatory, insecticidal, anti-malarial, and anti-Leishmania properties, as well as enhancing antigen-specific immune responses. The anti-inflammatory effects of 10-Hydroxydecanoic acid are primarily mediated by inhibiting the activation of NF-κB and the translation of interferon regulatory factor 1 (IRF-1), which reduces the production of interleukin 6 (IL-6) and nitric oxide (NO) in inflammatory cells. Additionally, 10-Hydroxydecanoic acid alleviates neuroinflammatory responses through the p53-autophagy pathway and the p53-NLRP3 pathway. Finally, 10-Hydroxydecanoic acid enhances antigen-specific immune responses by promoting the effective uptake of antigens by microfold cells.
    10-Hydroxydecanoic acid
  • HY-114360A
    Taurohyodeoxycholic acid sodium
    Inhibitor 99.60%
    Taurohyodeoxycholic acid (THDCA) sodium is the taurine-conjugated form of the secondary bile acid hyodeoxycholic acid. Taurohyodeoxycholic acid can also reduce the activity and expression of myeloperoxidase TNF-α and IL-6, as well as colonic damage in TNBS-induced ulcerative colitis mouse model.
    Taurohyodeoxycholic acid sodium
  • HY-P99273
    Vorsetuzumab
    Inhibitor 99.29%
    Vorsetuzumab (Anti-Human CD70 Recombinant Antibody) is a human anti-CD70 antibody. Vorsetuzumab enhances macrophage-related phagocytosis of renal carcinoma cells, shows inhibitory efficacy against Burkitt’s lymphoma.
    Vorsetuzumab
  • HY-P99148
    Anti-Mouse/Rat/Rabbit TNF alpha Antibody (TN3-19.12)
    Inhibitor
    Anti-Mouse/Rat/Rabbit TNF alpha Antibody (TN3-19.12) is an anti-mouse/rat/rabbit TNF alpha IgG antibody inhibitor derived from host Armenian Hamster.
    Anti-Mouse/Rat/Rabbit TNF alpha Antibody (TN3-19.12)
  • HY-P99742
    Mitazalimab
    Inhibitor 98.74%
    Mitazalimab (ADC-1013; JNJ-64457107) is FcγR-dependent CD40 agonist with tumor-directed activity. Mitazalimab activates antigen-presenting cells, e.g. dendritic cells (DC), to initiate tumor-reactive T cells. Therefore, Mitazalimab induces tumor-specific T cells to infiltrate and kill tumors. Mitazalimab remodels the tumor-infiltrating myeloid microenvironment.
    Mitazalimab
  • HY-B0367
    Lornoxicam
    Activator 99.36%
    Lornoxicam (Chlortenoxicam) is an orally active oxycontin nonsteroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory, antipyretic and anticancer activities. Lornoxicam exhibits good inhibitory effects on both COX-1 and COX-2 (COX-1: IC50=0.005 μM; COX-2:IC50=0.008 μM) and inhibits the production of NO by iNOS (IC50=65 μM) and the proinflammatory cytokine IL-6 (IC50=54 μM). Lornoxicam also inhibits tumor cell proliferation and migration and induces tumor cell apoptosis. Lornoxicam can be used in the study of inflammatory pain, colorectal cancer and breast cancer.
    Lornoxicam
  • HY-Y0399
    L-Norvaline
    Antagonist ≥98.0%
    L-Norvaline is the inhibitor for arginase, that promotes the production of NO, reduces oxidative stress, improves insulin resistance, and exhibits antioxidant and anti-hyperglycemic effects. L-Norvaline can be used in research of Alzheimer’s disease.
    L-Norvaline
  • HY-N9965
    2'-Fucosyllactose
    Inhibitor 99.95%
    2'-Fucosyllactose (2'-FL) is an oligosaccharide that could be derived from human milk. 2'-Fucosyllactose regulates the expression of CD14, alleviates colitis and regulates the gut microbiome. 2'-Fucosyllactose stimulates T cells to increase IFN-γ production and decreases IL-6, IL-17, and TNF-α production of cytokines.
    2'-Fucosyllactose
  • HY-150725C
    ODN 1585 sodium
    Inducer
    ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 sodium can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant.
    ODN 1585 sodium
  • HY-P9989
    Linvoseltamab
    Inhibitor 99.71%
    Linvoseltamab (REGN5458) is a bispecific T-cell engager (BiTE) antibody that specifically binds to B cell maturation antigen (BCMA) and CD3 of T cells, thereby directing T cells to multiple myeloma (MM) cells expressing BCMA and activating T cells to kill tumor cells. Linvoseltamab can be used in research of relapsed/refractory multiple myeloma (RRMM).
    Linvoseltamab
  • HY-119307
    Apratastat
    Inhibitor 99.67%
    Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC). Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Apratastat
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. 
 

TNFRSF1A/CD120a

TNFRSF5/CD40

TNFRSF6/Fas/CD95

TNFRSF7/CD27

TNFRSF8/CD30

TNFRSF9/4-1BB/CD137

TNFRSF16/NGF Receptor/CD271

TNFRSF18/GITR/CD357

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TNF Receptor Inhibitors, Agonists, Antagonists & Activators
Product NameTNFRSF1A/CD120aTNFRSF5/CD40TNFRSF6/Fas/CD95TNFRSF7/CD27TNFRSF8/CD30TNFRSF9/4-1BB/CD137TNFRSF16/NGF Receptor/CD271TNFRSF18/GITR/CD357Purity    
Etanercept  
Fas
     99.20%
R-7050 
CD40
      99.96%
Oxazolone
TNFR1
       ≥98.0%
Utomilumab     
4-1BB
  99.33%
TNF-α-IN-2 
CD40, IC50: 25 nM
      98.75%
Brentuximab    
CD30
   99.64%
BIO8898 
CD40L, IC50: 25 μM
      99.88%
Golimumab 
CD40
      99.71%
KR-33493  
Fas
     99.94%
Iscalimab 
CD40, IC50: 0.3 nM
      99.64%
Taurohyodeoxycholic acid sodium
TNFR1
       99.60%
Mitazalimab 
CD40
      98.74%
Toralizumab 
CD40L
      99.57%
Lucatumumab 
CD40
      98.18%
Ragifilimab       
GITR
GSK2245035 
CD40, pEC50: 6.5
      99.85%
DRI-C25441 
CD40, IC50: 0.36 μM
      99.53%
AQX-016A 
CD40
      98.00%
HDMAPP triammonium
TNFRSF1A
       
Letolizumab 
CD40L
      
Cinrebafusp alfa     
4-1BB, Kd: 5 nM
  98.53%
Ravagalimab 
CD40, EC50: 3.7 nM
      99.31%
DRI-C21041 
CD40L, IC50: 0.31 μM
      
Anti-inflammatory agent 17 
TNF-α, IC50: 2.576 μM
      
Relfovetmab      
NGF
 
Ranevetmab      
NGF
 
TNF-α-IN-14 
TNF-α, IC50: 1.1 μM
      
Semapimod 
CD40
      
MG-C-30   
CD27, EC50: 0.84 μM
    
Tecaginlimab 
CD40
   
4-1BB
  99.00%
(E)-C-HDMAPP ammonium
TNFRSF1A
       
TNF-α-IN-15 
TNF-α
      
TNF-α-IN-12 
TNF-α
      
Cudraflavone B
TNFRSF1A