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-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-P991149
    Nesfrotamig
    Inhibitor
    Nesfrotamig is a humanized immunoglobulin (H-γ1-scFv-L-κ) dimer monoclonal antibody targeting human epidermal growth factor receptor 2 (ERBB2) and human tumor necrosis factor receptor superfamily member 9 (TNFRSF9). Nesfrotamig is promising for research of cancers, especially in ERBB2-positive related tumor diseases, such as breast cancer and gastric cancer.
    Nesfrotamig
  • 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-P991455
    PTX-35
    Agonist
    PTX-35 is a human IgG monoclonal antibody (mAb) targeting TNFRSF25. PTX-35 reduces the suppressive activity of regulatory T cells and enhances CD4+ T cell effector responses in a mouse melanoma model. PTX-35 can be used in Islet cell transplant rejection and Solid tumours research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).
    PTX-35
  • 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.
    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
  • HY-131528
    Tenilsetam
    Tenilsetam (CAS 997) is an antidementia compound. Tenilsetam is an advanced glycation end product (AGE) inhibitor. Tenilsetam inhibits early retinopathy in experimental diabetes rats.
    Tenilsetam
  • HY-N0604R
    Ginsenoside Rh1 (Standard)
    Inhibitor
    Ginsenoside Rh1 (Standard) is the analytical standard of Ginsenoside Rh1. This product is intended for research and analytical applications. Ginsenoside Rh1 (Prosapogenin A2) inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
    Ginsenoside Rh1 (Standard)
  • HY-P990738
    Enristomig
    Enristomig is an anti-TNFRSF9/CD274 monoclonal antibody.
    Enristomig
  • HY-P991155
    Ramantamig
    Inhibitor
    Ramantamig is a humanized monoclonal antibody targeting human CD3ε, GPRC5D, and TNFRSF17 (tumor necrosis factor receptor superfamily member 17)。Ramantamig is promising for research of cancers, especially hematological malignancies such as multiple myeloma.
    Ramantamig
  • HY-171658
    R1-ICR-5
    Inhibitor
    R1-ICR-5 is a selective PROTAC degrader that targets serine/threonine-protein kinase 1 (RIPK1). R1-ICR-5 mediates the degradation of RIPK1 through VHL, thereby deregulating the TNFR1 and TLR3/4 signaling hubs, enhancing the output of NF-κB, MAPK, and IFN signaling, and simultaneously promoting the activation of RIPK3 and the induction of necroptosis. R1-ICR-5 is promising for research of cancers and inflammatory diseases. (Pink: PK68 (HY-128348); Black: linker (HY-W012241); Blue: (S,R,S)-AHPC (HY-125845).
    R1-ICR-5
  • HY-157809
    Anti-inflammatory agent 74
    Inhibitor
    Anti-inflammatory agent 74 (B5) is an anti-inflammatory agent that can inhibit NO, IL-6, and TNF-α, with IC50 values of 10.88 μM and 4.93 μM for NO and IL-6, respectively. Anti-inflammatory agent 74 alleviates acute lung injury (ALI) by regulating inflammatory mediators and inhibiting the MAPK and NF-κB signaling pathways.
    Anti-inflammatory agent 74
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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