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-148908
    TNF-α-IN-8
    Inhibitor
    TNF-α-IN-8 (compound I-42) is a TNF-α inhibitor. TNF-α-IN-8 is an isoindole-imide compound. TNF-α-IN-8 can be used for the research of cancer, heart disease, osteoporosis, inflammatory, allergic and autoimmune diseases. TNF-α-IN-8 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    TNF-α-IN-8
  • HY-15509
    Semapimod
    Inhibitor
    Semapimod, an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod has potential in a variety of inflammatory and autoimmune disorders.
    Semapimod
  • HY-P990710
    Acimtamig
    Acimtamig (AFM13) is a CD30/CD16A bispecific innate cell engager. Acimtamig binds to the CD16A expressed on natural killer (NK) cells and binds to CD30 on CD30-expressing tumor cells, thereby selectively cross-linking tumor and NK cells. Acimtamig can be used for the study of eripheral T-cell lymphoma (PTCL).
    Acimtamig
  • HY-159886
    MG-C-30
    Agonist
    MG-C-30 is an orally active agonist for CD27 with an EC50 of 0.84 μM. MG-C-30 activates NK cells and T cell co-stimulatory signals, and enhances immune response. MG-C-30 exhibits antitumor efficacy in mouse EG7-OVA model.
    MG-C-30
  • HY-P99692
    Lenercept
    Inhibitor
    Lenercept (Ro 45-2081) is a recombinant fusion protein that consists of the soluble TNF-receptor (p55) linked to the Fc portion of human IgG1.
    Lenercept
  • HY-P99572
    Tecaginlimab
    Inhibitor 99.00%
    Tecaginlimab (BNT-312) is a Fc-inert bispecific antibody for dual targeting and conditional stimulation of CD40 and 4-1BB. Tecaginlimab can enhance priming and reactivation of tumor-specific immunity.
    Tecaginlimab
  • HY-P3149
    LEESGGGLVQPGGSMK
    LEESGGGLVQPGGSMK, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α.
    LEESGGGLVQPGGSMK
  • HY-168935
    Anti-inflammatory agent 95
    Inhibitor
    Anti-inflammatory agent 95 (Compound 2e) is an anti-inflammatory agent that exhibits the most potent anti-inflammatory activity in LPS (HY-D1056)-induced RAW 264.7 mouse macrophages. It significantly inhibits the production of NO, with an IC50 of 8.8 μM, and reduces the secretion of TNF-α and IL-1β, with inhibition rates reaching 60% and over 90%, respectively, at a concentration of 100 μM. Anti-inflammatory agent 95 holds promise for research in the field of inflammatory diseases.
    Anti-inflammatory agent 95
  • HY-N0507R
    Rosavin (Standard)
    Inhibitor
    Rosavin (Standard) is the analytical standard of Rosavin. This product is intended for research and analytical applications. Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis.
    Rosavin (Standard)
  • HY-N0261R
    Aurantio-obtusin (Standard)
    Inhibitor
    Aurantio-obtusin (Standard) is the analytical standard of Aurantio-obtusin. This product is intended for research and analytical applications. Aurantio-obtusin is a anthraquinone compound that can be extracted from cassia seed. Aurantio-obtusin has the effects of decreasing blood pressure, decreasing blood lipids and anti-inflammatory.Aurantio-obtusin is an orally active vasodilator. Aurantio-obtusin ameliorates hepatic steatosis through AMPK/ autophagy-and AMPK/TFEB mediated inhibition of lipid accumulation.
    Aurantio-obtusin (Standard)
  • HY-P10551
    Apo A-I mimetic 5A peptide
    Inhibitor
    Apo A-I mimetic 5A peptide is a synthetic peptide molecule designed based on the structure and function of naturally occurring apolipoprotein A-I (Apo A-I). Apo A-I mimetic 5A peptide can promote the efflux of cholesterol from cells and help reduce the accumulation of cholesterol in cells. Apo A-I mimetic 5A peptide also shows anti-inflammatory activity and can reduce inflammatory markers in blood and tissues. Apo A-I mimetic 5A peptide can be used in the study of cardiovascular diseases.
    Apo A-I mimetic 5A peptide
  • HY-P10693
    CZEN-002
    Inhibitor
    CZEN-002 is a derivative of alpha-melanocyte-stimulating hormone that has anti-inflammatory and antibacterial properties, inhibiting the production of TNF-α.
    CZEN-002
  • HY-P1700
    BCMA72-80
    BCMA72-80 is a HLA-A2-specific B-cell maturation antigen (BCMA) peptide, with great affinity to HLA-A2, used in the research of multiple myeloma or other B-cell maturation antigen expressing tumors.
    BCMA72-80
  • HY-P990530
    Anti-TNFSF2/TNFa Antibody (hMAK195)
    Anti-TNFSF2/TNFa Antibody (hMAK195) is a human antibody expressed in CHO cells that targets TNFSF2/TNFa. Anti-TNFSF2/TNFa Antibody (hMAK195) has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145.06 kDa. The isotype control for Anti-TNFSF2/TNFa Antibody (hMAK195) can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-TNFSF2/TNFa Antibody (hMAK195)
  • HY-107352S
    Fosfenopril-d7
    Fosfenopril-d7 is deuterium labeled Fosfenopril.
    Fosfenopril-d<sub>7</sub>
  • HY-111326S
    Naphazoline-d4 hydrochloride
    Naphazoline-d4 (hydrochloride) is the deuterium labeled Naphazoline hydrochloride[1].
    Naphazoline-d<sub>4</sub> hydrochloride
  • HY-134950
    (E)-C-HDMAPP ammonium
    Activator
    (E)-C-HDMAPP ammonium, is a potent phosphoantigen in ammonium form as well as a pyrophosphonate form of (E)-HDMAPP. (E)-C-HDMAPP is also an effective activator of γδ-T cells, induces T-cell stimulatory responses in vitro (EC50=0.91 nM for TNF-α release).
    (E)-C-HDMAPP ammonium
  • HY-123568
    PBI-1393
    Inhibitor
    PBI-1393 (BCH-1393) is an anticancer agent that enhances Th1 type cytokine production and primary T cell activation.
    PBI-1393
  • HY-144727
    Anti-inflammatory agent 11
    Inhibitor
    Anti-inflammatory agent 11 (compound 16) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 11 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 1.3 and 6.9 μM, respectively. Anti-inflammatory agent 11 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 11 can be used for tuberculosis (TB) research.
    Anti-inflammatory agent 11
  • HY-106215
    Etiprednol dicloacetate
    Inhibitor
    Etiprednol dicloacetate (BNP 166) is an anti-inflammatory agent. Etiprednol dicloacetate inhibits eosinophil accumulation. Etiprednol dicloacetate can be used in the research of inflammatory airway diseases, such as asthma.
    Etiprednol dicloacetate
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