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-160435
    TNF-α-IN-14
    Inhibitor
    TNF-α-IN-14 is a potent and selective TNFα inhibitor with an IC50 value of 1.1 µM. TNF-α-IN-14 shows antiinflammatory properties (WO2001072735A2; compound 12).
    TNF-α-IN-14
  • HY-P99653A
    Ianalumab (FUT8-KO)
    Inhibitor
    Ianalumab (FUT8-KO) is an anti-BAFF-R monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Ianalumab (FUT8-KO) can block the interaction between BAFF and BAFF-R and antagonize the apoptosis protection mediated by BAFF.
    Ianalumab (FUT8-KO)
  • HY-B1201R
    Tiratricol (Standard)
    Inhibitor
    Tiratricol (Standard) is the analytical standard of Tiratricol. This product is intended for research and analytical applications. Tiratricol is an orally available thyroid hormone analog that inhibits pituitary thyroid-stimulating hormone secretion. Tiratricol is an intracellular toxin neutralizer that inhibits LPS and lipid A cytotoxicity with IC50s of 20 μM and 32 μM, respectively. Tiratricol reduces TNF production in lipopolysaccharide-stimulated macrophages. Tiratricol also has antiviral activity and is an inhibitor of yellow fever virus (Flavivirus). It can bind to the RdRp domain of the viral NS5 protein to hinder YFV replication..
    Tiratricol (Standard)
  • HY-N0509R
    Astilbin (Standard)
    Inhibitor
    Astilbin (Standard) is the analytical standard of Astilbin. This product is intended for research and analytical applications. Astilbin is a flavonoid compound and enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.
    Astilbin (Standard)
  • HY-12085S2
    (Rac)-Apremilast-d5
    (Rac)-Apremilast-d5 is a deuterium labeled (R)-Apremilast. (R)-Apremilast ((R)-CC-10004) is a enantiomer of Apremilast[1].
    (Rac)-Apremilast-d<sub>5</sub>
  • HY-P990270
    Anti-Mouse CD40L/CD154 (D265A) Antibody (MR-1)
    Anti-Mouse CD40L/CD154 (D265A) Antibody (MR-1) is a mouse-derived IgG1, κ type antibody inhibitor, targeting to mouse CD40L/CD154.
    Anti-Mouse CD40L/CD154 (D265A) Antibody (MR-1)
  • HY-151188
    DHU-Se1
    Inhibitor
    DHU-Se1 is a potent anti-inflammatory agent. DHU-Se1 can stimulate macrophages to release the reactive selenium compound and reduce the expression of cellular inflammatory factors (eg: iNOS and TNF-α). DHU-Se1 alleviate the process of inflammation by blocking the polarization of macrophages from M0 to M1.
    DHU-Se1
  • HY-P99775
    Placulumab
    Inhibitor
    Placulumab (ART621) is an anti-TNF α monoclonal antibody. Placulumab has anti-inflammatory activity and has potential applications in inflammatory diseases such as arthritis.
    Placulumab
  • HY-N2119R
    Sciadopitysin (Standard)
    Sciadopitysin (Standard) is the analytical standard of Sciadopitysin. This product is intended for research and analytical applications. Sciadopitysin is a type of biflavonoids in leaves from ginkgo biloba. Sciadopitysi inhibits RANKL-induced osteoclastogenesis and bone loss by inhibiting NF-κB activation and reducing the expression of c-Fos and NFATc1.
    Sciadopitysin (Standard)
  • HY-155820
    Anti-inflammatory agent 54
    Inhibitor
    Anti-inflammatory agent 54 (compound 9c) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 2.4 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model.
    Anti-inflammatory agent 54
  • HY-Y0148R
    10-Hydroxydecanoic acid (Standard)
    Inhibitor
    10-Hydroxydecanoic acid (Standard) is the analytical standard of 10-Hydroxydecanoic acid. This product is intended for research and analytical applications. 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[1][2][3][4][5].
    10-Hydroxydecanoic acid (Standard)
  • HY-N0512R
    Loganin (Standard)
    Inhibitor
    Loganin (Standard) is the analytical standard of Loganin. This product is intended for research and analytical applications. 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 (Standard)
  • 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-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)
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%
BIO8898 
CD40L, IC50: 25 μM
      99.88%
Brentuximab    
CD30
   99.64%
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
      99.23%
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