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-N15589
    8-(6,7-Dihydroxy-3,7-dimethyl-2E-octenyloxy)psoralen
    Inhibitor
    8-(6,7-Dihydroxy-3,7-dimethyl-2E-octenyloxy)psoralen is a compound found in Citrus grandis. 8-(6,7-Dihydroxy-3,7-dimethyl-2E-octenyloxy)psoralen has significant anti-inflammatory activity, which mainly works by inhibiting the secretion of inflammatory factors IL-1β, PGE2 and TNF-α. 8-(6,7-Dihydroxy-3,7-dimethyl-2E-octenyloxy)psoralen can be used in the study of inflammation.
    8-(6,7-Dihydroxy-3,7-dimethyl-2E-octenyloxy)psoralen
  • HY-173334
    hMAO-B-IN-11
    Inhibitor
    hMAO-B-IN-11 (Compound 12) is a selective and reversible inhibitor of human monoamine oxidase B (hMAO-B) with an IC50 of 0.11 µM. hMAO-B-IN-11 acts through competitive binding to the hMAO-B active site, preventing oxidative deamination of monoamines and reducing hydrogen peroxide production. hMAO-B-IN-11 also inhibits pro-inflammatory mediators (NO, TNF-α, IL-1β) in activated microglia, hMAO-B-IN-11 is promising for research of neurodegenerative diseases like Parkinson’s and Alzheimer’s.
    hMAO-B-IN-11
  • HY-160027
    TNF-alpha-IN-1
    Inhibitor
    TNF-alpha-IN-1 (compound 202) is an orally active inhibitor of TNF-alpha. TNF-alpha-IN-1 has anti-inflammatory activity which can used in study rheumatoid arthritis, psoriasis, and asthma.
    TNF-alpha-IN-1
  • HY-108162A
    Ataquimast
    Inhibitor
    Ataquimast is a COX-2 inhibitor that inhibits the release of leukotrienes, TNF-α and GM-CSF. Ataquimast can be used in the study of advanced receptor-positive breast cancer.
    Ataquimast
  • HY-P11098
    Peptide HV2
    Inhibitor
    Peptide HV2 is an antibiotic that exerts anti-inflammatory effects by inhibiting TNF-α. Peptide HV2 has antibacterial activity.
    Peptide HV2
  • HY-164893
    ABBV-154
    Inhibitor
    ABBV-154 is an anti-TNF antibody-drug conjugate (ADC). ABBV-154 is composed of the humanized antibody Adalimumab (HY-P9908) conjugated with a glucocorticoid receptor modulator (HY-137883). ABBV-154 can be used in studies of rheumatoid arthritis, Crohn's disease and polymyalgia rheumatica.
    ABBV-154
  • HY-P991465
    Anti-CD27 Antibody (M2177)
    Inhibitor
    Anti-CD27 Antibody (M2177) is a human monoclonal antibody (mAb) targeting TNFRSF7/CD27. Anti-CD27 Antibody (M2177) inhibits the binding of sCD70 to human CD27 ECD-Fc. Anti-CD27 Antibody (M2177) can be used in the study of anti-tumor immunity. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-CD27 Antibody (M2177)
  • HY-126232
    Verproside
    Inhibitor
    Verproside, a catalpol derivative iridoid glycoside isolated from the genus Pseudolysimachion, represses TNF-α -induced MUC5AC expression by inhibiting NF-κB activation via the IKK/IκB signaling cascade. Verproside has potent anti-inflammatory, antioxidant, antinociceptive and anti-asthmatic activities. Verproside has the potential for the study of chronic obstructive pulmonary disease (COPD).
    Verproside
  • HY-W338346
    Salicylate choline
    Inhibitor
    Salicylate choline is an orally active derivative of Aspirin (acetylsalicylic acid) (HY-14654). Salicylate choline significantly reduces IL-1β, IL-6, TNF-α and IL-10 levels in cells. Salicylate choline enhances the anti-tumor activity of the CRM1 inhibitor Selinexor (KPT-330) (HY-17536) through inducing S-phase cell cycle arrest and impairing DNA damage repair. Salicylate choline combined with Selinexor demonstrates excellent anti-tumor efficacy in mice xenograft model harboring JeKo-1 cells. Salicylate choline can be used for the study of rheumatic diseases, inflammation and cancer.
    Salicylate choline
  • HY-N0201R
    Atractylenolide I (Standard)
    Atractylenolide I (Standard) is the analytical standard of Atractylenolide I. This product is intended for research and analytical applications. Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
    Atractylenolide I (Standard)
  • HY-N3421
    Koaburaside
    Inhibitor
    Koaburaside is a cytoprotective and anti-inflammatory natural compound. Koaburaside shows antioxidant activity with an IC50 of 9.0 μM for DPPH-free radical scavenging assay. Koaburaside inhibits histamine release and expressions of IL-6 and TNF-α in human mast cells. Koaburaside also effectively inhibits influenza A neuraminidase.
    Koaburaside
  • HY-175250
    TNF-α-IN-25
    Inhibitor
    TNF-α-IN-25 is an orally active TNF-α inhibitor. TNF-α-IN-25 shows Fluorescence Polarization (FP) assay IC50 of 103 nM in FP binding assays and L929 assay IC50 of 505 nM in cell-based assays. TNF-α-IN-25 inhibits paw swelling in the glucose-6-phosphate isomerase (GPI) arthritis model. TNF-α-IN-25 can be used for the study of arthritis.
    TNF-α-IN-25
  • HY-171837A
    t9,t11,c15-CLNA
    Inhibitor
    t9,t11,c15-CLNA is a conjugated linolenic acid (CLNA) isomer produced by Lactobacillus plantarum ZS2058. t9,t11,c15-CLNA has the main activities of anti-inflammatory, antioxidant and improving intestinal barrier function. The regulatory mechanism of t9,t11,c15-CLNA includes upregulation of tight junction proteins, inhibition of pro-inflammatory cytokines (such as TNF-α, IL-6) and activation of antioxidant enzymes (such as SOD, CAT). t9,t11,c15-CLNA can be used in the study of inflammatory bowel diseases (such as colitis).
    t9,t11,c15-CLNA
  • HY-172111
    EGFR-IN-144
    Antagonist
    EGFR-IN-144 (Compound 4B) exhibits inhibitory activities against EGFR (IC50=0.639 µg/mL) and tubulin polymerization (IC50=7.339 µg/mL). EGFR-IN-144 exhibits cytotoxicity in multiple cancer cell with GI50 of nanomolare levels. EGFR-IN-144 downregulates the expressions of mTOR, TNF-α, and IL-6, arrests the cell cycle at G1/S phase, and induces apoptosis.
    EGFR-IN-144
  • HY-P990304B
    Anti-Mouse 4-1BBL/CD137L (D265A) Antibody (TKS-1)
    Inhibitor
    Anti-Mouse 4-1BBL/CD137L (D265A) Antibody (TKS-1) is a mouse-derived IgG1 κ antibody inhibitor that targets mouse 4-1BBL/CD137L. Anti-Mouse 4-1BBL/CD137L (D265A) Antibody (TKS-1) is a chimeric version of the original TKS-1 antibody (HY-P990304). The variable domain sequences are identical to the original TKS-1 but the constant region sequences have been switched from rat IgG2a to mouse IgG1. Anti-Mouse 4-1BBL/CD137L (D265A) Antibody (TKS-1) contains a D265A mutation in the Fc fragment rendering it unable to bind to endogenous Fcγ receptors. Anti-Mouse 4-1BBL/CD137L (D265A) Antibody (TKS-1) reacts with mouse 4-1BB ligand (4-1BBL). Anti-Mouse 4-1BBL/CD137L (D265A) Antibody (TKS-1) can be used for the researches of cancer, infection, inflammation and immunology.
    Anti-Mouse 4-1BBL/CD137L (D265A) Antibody (TKS-1)
  • HY-118250A
    GSK2245035 maleate
    Activator
    GSK2245035 maleate is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 maleate has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 maleate effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 maleate is used for asthma.
    GSK2245035 maleate
  • HY-P990241
    Anti-Mouse GITR (D265A) Antibody (DTA-1)
    Agonist
    Anti-Mouse GITR (D265A) Antibody (DTA-1) is an anti-mouse GITR IgG1 monoclonal antibody. Anti-Mouse GITR (D265A) Antibody (DTA-1) is a chimeric antibody of the original DTA-1 antibody (HY-P990124). Anti-Mouse GITR (D265A) Antibody (DTA-1) contains the D265A mutation region. Anti-Mouse GITR (D265A) Antibody (DTA-1) can be used for research on cancer and allergic conditions. The recommed isotype control of Anti-Mouse GITR (D265A) Antibody (DTA-1) is Mouse IgG1 kappa, Isotype Control (HY-P99977).
    Anti-Mouse GITR (D265A) Antibody (DTA-1)
  • HY-P990249
    Anti-Mouse DR5/CD262 Antibody (MD5-1)
    Inhibitor
    Anti-Mouse DR5/CD262 Antibody (MD5-1) is an anti-mouse DR5/CD262 IgG monoclonal antibody. Anti-Mouse DR5/CD262 Antibody (MD5-1) can eliminate myeloid derived suppressor cells (MDSCs) and enhance T cell anti-tumor immunity. Anti-Mouse DR5/CD262 Antibody (MD5-1) can be used for research on cancer such as gastric and colon cancer.
    Anti-Mouse DR5/CD262 Antibody (MD5-1)
  • HY-162850
    DOR agonist 2
    Inhibitor
    DOR agonist 2 (Compound 3) is a Delta Opioid Receptor agonist. DOR agonist 2 can inhibit the expression of TNF-α, prevent NF-κB transport to the nucleus, and activate the G protein-mediated ERK1/2 pathway. DOR agonist 2 can be used in the study of neurodegenerative diseases.
    DOR agonist 2
  • HY-178037
    TLR9 antagonist 1
    Inhibitor
    TLR9 antagonist 1 (Compound 38) is a selective TLR9 antagonist with an IC50 of 0.1  nM for hTLR9 over hTLR2/4/5/7/8. TLR9 antagonist 1 exacerbates disease symptoms with increased anti-dsDNA and anti-Sm levels in systemic lupus erythematosus (SLE) mouse models. TLR9 antagonist 1 can be used for inflammatory and immune diseases like lupus and arthritis research.
    TLR9 antagonist 1
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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