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-P991012
    Nuvustotug
    Inhibitor
    HY-P991012 is an TNFRSF4-targeting IgG1κ type human antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Nuvustotug
  • HY-P991014
    Pamlectabart
    Inhibitor
    HY-P991014 is an TNFRSF17-targeting IgG1κ type humanized antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Pamlectabart
  • HY-N7513R
    Homovanillyl alcohol (Standard)
    Orphenadrine (hydrochloride) (Standard) is the analytical standard of Orphenadrine (hydrochloride). This product is intended for research and analytical applications. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases.
    Homovanillyl alcohol (Standard)
  • HY-P990971
    Atenastobart
    Inhibitor
    HY-P990971 is an TNFRSF9-targeting IgG1λ2 type human antibody, the recommed isotype control is Human IgG1 lambda2, Isotype Control (HY-P990096).
    Atenastobart
  • HY-P991036
    Velinotamig
    Inhibitor
    HY-P991036 is an CD3E/TNFRSF17-targeting H-γ1_L-κ/H-γ1_L-κ type bispecific antibody.
    Velinotamig
  • HY-B0809A
    Theophylline monohydrate
    Inhibitor
    Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline monohydrate
  • HY-P99470
    Benufutamab
    Agonist 98.62%
    Benufutamab (GEN1029) is a death receptor 5 (DR5)-specific agonistic antibody. Benufutamab is a mixture of 2 noncompeting DR5-specific IgG1 antibodies, each with an E430G mutation in the Fc domain. Benufutamab has antitumor effects.
    Benufutamab
  • HY-P990901
    Aplitabart
    Inhibitor
    HY-P990901 is an TNFRSF10B-targeting IgM-κ type humanized antibody.
    Aplitabart
  • HY-P990939
    Podentamig
    Inhibitor
    HY-P990939 is an CD3E/TNFRSF17-targeting VH-VH'-(scFv-heavy -λ) type chimeric antibody.
    Podentamig
  • HY-P99782
    Opinercept
    Inhibitor
    Opinercept is a recombinant fusion protein comprising an TNFRSF1B fused to a human IgG1 Fc. Opinercept is a tumor necrosis factor-alpha (TNF-alpha) inhibitor. Opinercept can be used for the research of rheumatoid arthritis (RA).
    Opinercept
  • HY-P99578
    Tanfanercept
    Inhibitor
    Tanfanercept (HL036337) is an TNF-α receptor fusion protein that targets TNF-α. Tanfanercept is effective in ameliorating corneal erosions in a dry eye (DE) mouse model.
    Tanfanercept
  • HY-P990980
    Cizutamig
    Inhibitor
    HY-P990980 is an TNFRSF17-targeting [L-κ-H-γ1_[VH-G1(CH1-h)]_Lκ] dimer type humanized antibody.
    Cizutamig
  • HY-P99704
    Licaminlimab
    Inhibitor
    Licaminlimab (OCS-02) is a single-chain anti-TNF alpha antibody fragment. TNF alpha is an inflammatory cytokine produced by macrophages and monocytes during inflammation.
    Licaminlimab
  • HY-P991003
    Ingitamig
    Inhibitor
    HY-P991003 is an TNFRSF17/KLRK1-targeting (G1_L-κ)_(G1-scFvkh_L-κ) type bispecific antibody.
    Ingitamig
  • HY-P99565
    Tengonermin
    Inhibitor
    Tengonermin (ARENEGYR) is a vascular-targeting agent consisting of the human Tumour Necrosis Factor-α (TNF-α) conjugated with the CNGRCG peptide. Tengonermin increases penetration of intratumoral chemotherapy and T-cell infiltration by modifying the tumour microenvironment.
    Tengonermin
  • HY-P990531
    Anti-TNFSF9/4-1BBL Antibody
    The Anti-TNFSF9/4-1BBL Antibody is a CHO-expressed humanized antibody that targets TNFSF9/4-1BBL. The Anti-TNFSF9/4-1BBL Antibody has huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 150 kDa. For isotype control of the Anti-TNFSF9/4-1BBL Antibody, you can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-TNFSF9/4-1BBL Antibody
  • HY-160437
    TNF-α-IN-16
    Inhibitor
    TNF-α-IN-16 is a potent TNFα inhibitor with an IC50 of <0.6 μM. TNF-α-IN-16 has antiinflammatory properties (WO2001072735A2; example 18).
    TNF-α-IN-16
  • HY-W012732R
    Isoquinoline (Standard)
    Inhibitor
    Isoquinoline (Standard) is the analytical standard of Isoquinoline. This product is intended for research and analytical applications. Isoquinoline is an analog of pyridine. Isoquinoline structural-based alkaloids, such as tropoloisoquinoline, phthalideisoquinoline, and naphthylisoquinoline has anti-cancer activities.
    Isoquinoline (Standard)
  • HY-170492
    sEH inhibitor-19
    Antagonist
    sEH inhibitor-19 (Compound (R)-14i) is an orally active inhibitor for soluble epoxide hydrolase (sEH) with an IC50 of 1.2 nM. sEH inhibitor-19 inhibits the expression of TNF-α and IL-6, exhibits anti-inflammatory activity in mouse acute pancreatitis or Carrageenan (HY-125474)-induced edema models.
    sEH inhibitor-19
  • HY-P990559
    BMS-986178
    BMS-986178 is a humanized antibody expressed in CHO, targeting TNFRSF4/OX40/CD134. BMS-986178 has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for BMS-986178 can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    BMS-986178
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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