TNF Receptor

Receptor

Tumor Necrosis Factor Receptor; TNFR

TNF Receptor

TNF Receptor Isoform Specific Products:

TNF Receptor Related Products (545)
Recombinant Proteins (237)
Antibodies (23)
TNF Receptor Signaling Pathway
TNF Receptor Isoform Comparison

By Effects:	Controls (3) Inhibitors (387) Agonists (13) Antagonists (14) Activators (24) Modulators (6) Inducers (6)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-120934

C25-140	Inhibitor	99.92%
C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity.

HY-133122

UCB-9260	Inhibitor	98.38%
UCB-9260, an orally active compound, inhibits TNF signaling by stabilising an asymmetric form of the trimer.?UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar?K_d?of 13?nM.

HY-B0190A

Nafamostat mesylate		99.85%
Nafamostat mesylate (FUT-175), an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat mesylate has anticancer and antivirus effect. Nafamostat mesylate induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat mesylate can be used in the development of the pathological thickening of the arterial wall.

HY-13812

QNZ	Inhibitor	99.50%
QNZ (EVP4593) shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC₅₀s of 11 and 7 nM, respectively. QNZ (EVP4593) is a neuroprotective inhibitor of SOC channel.

HY-126360

Oxazolone	Activator	≥98.0%
Oxazolone is a haptenizing agent that induces acute or chronic inflammation of the large intestine and is used to construct models of colitis. Oxazolone can cause Th1/Th2-dependent colitis with weight loss and diarrhea. Oxazolone-induced inflammation can be mitigated by neutralizing anti-IL-4 or anti-TNF-α antibodies or decoy IL-13R2-α-FC proteins.

HY-N0201

Atractylenolide I		99.94%
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.

HY-P99056

Utomilumab	Inhibitor	99.33%
Utomilumab (PF 05082566) is a fully human IgG2 mAb agonist of the T-cell costimulatory receptor 4-1BB/CD137. Utomilumab can be used for the research of relapsed/refractory follicular lymphoma (FL) and other CD20⁺ non-Hodgkin lymphomas (NHL).

HY-B0539

Desloratadine	Inhibitor	99.83%
Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (K_i=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria.

HY-N0297

Sinensetin	Inhibitor	99.87%
Sinensetin is a methylated flavonoid found in fruits that has strong anti-vascular and anti-inflammatory properties.

HY-P9952

Belimumab	Inhibitor	99.40%
Belimumab (LymphoStat B) is a humanized IgG1λ monoclonal antibody against B-lymphocyte stimulator (BLyS) protein. Belimumab antagonizes BLyS activity in autoimmune diseases and B-lymphocyte malignancies. Belimumab can be used for systemic lupus erythematosus (SLE) research.

HY-P9953

Certolizumab pegol	Inhibitor	99.30%
Certolizumab pegol (Certolizumab) is a recombinant, polyethylene glycolylated, antigen-binding fragment of a humanized monoclonal antibody that selectively targets and neutralizes tumour necrosis factor-α (TNF-α). Certolizumab pegol can be used for rheumatoid arthritis and Crohn disease research.

HY-N0029

Forsythoside B		99.99%
Forsythoside B is a phenylethanoid glycoside isolated from Forsythia suspensa (Thunb.) Vahl, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.

HY-P9980

Belantamab	Inhibitor	99.90%
Belantamab (GSK2857916) is a humanized IgG1 anti-BCMA/TNFRSF17 monoclonal antibody. Belantamab is linked to MMAF (HY-15579) through a non-cleavable ADC linker to synthesize the antibody-active molecule conjugate (ADC) Belantamab mafodotin (HY-P3239). After binding to BCMA on the surface of tumor cells, Belantamab mafodotin enters the cell through receptor-mediated endocytosis. After entering the cell, Belantamab mafodotin releases MMAF, blocks cell division by inhibiting tubulin polymerization, arrests the cell cycle and induces cell apoptosis. Belantamab can be used for the study of multiple myeloma, especially relapsed/refractory multiple myeloma.

HY-P9979

Rozanolixizumab	Inhibitor	99.34%
Rozanolixizumab (UCB7665), a humanized high-affinity anti-human neonatal Fc receptor (FcRn) monoclonal antibody (IgG4P), is used to the research of reducing pathogenic IgG in autoimmune and alloimmune diseases.

HY-N0633

Muscone	Inhibitor	≥98.0%
Muscone is the main active monomer of traditional Chinese medicine musk. Muscone inhibits NF-κB and NLRP3 inflammasome activation. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6), and ultimately improves cardiac function and survival rate.

HY-122663A

BIO8898	Inhibitor	99.88%
BIO8898 is a potent CD40-CD154 inhibitor. BIO8898 inhibits soluble CD40L binding to CD40-Ig with an IC₅₀ value of 25 µM. BIO8898 inhibits CD40L-induced apoptosis.

HY-134471

TNF-α-IN-2	Inhibitor	98.75%
TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC₅₀ of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis.

HY-P990008

Atrosab	Antagonist	98.00%
Atrosab is a humanized IgG1 antagonistic anti-TNFR1 antibody. Atrosab inhibits TNF-mediated Apoptosis induction and IL-6 and IL-8 production. Atrosab reduces neurological deficits. Atrosab can be used for research of inflammatory disease. The recommend isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).

HY-111255

SPD304	Inhibitor	99.58%
SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC₅₀ of 22 μM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.

HY-N6796

Manumycin A	Inhibitor	99.27%
Manumycin A is a polyketide antibiotic and an inhibitor of thioredoxin reductase 1 (TrxR-1). Manumycin A can inhibit the growth of breast cancer cells and exert its anti-tumor activity through LC3. Manumycin A can downregulate the release of pro-inflammatory cytokines in human monocytes stimulated by TNF α, and has potential anti-inflammatory activity. Manumycin A can inhibit the Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration resistant prostate cancer cells to suppress exosome biogenesis and secretion.

TNF RIPK1 TRADD TRAF2/5 cIAP1/2 TNFR1 LUBAC TAB2 TAB3 TAK1 IKKβ NEMO IKKα RIPK1 CYLD RIPK1 RIPK1 TRADD FADD FADD Pro-caspase 8 Pro-caspase 8 Pro-caspase 8 Pro-caspase 8 Pro-caspase 8 Pro-caspase 8 Pro-caspase 8 Pro-caspase 8 Pro-caspase 8 Active
Caspase 8 Caspase 3/7 RIPK1 or
RIPK3 RIPK1 RIPK3 Apoptosis FADD RIPK1 RIPK3 FADD FLIP_L FLIP_L RIPK1 or
RIPK3 FLIP_L or FLIP_S FADD FADD RIPK1 RIPK3 RIPK3 RIPK3 MLKL MLKL MLKL AP1 TRAF1/2 cIAP1/2 MKK3 MKK1/7 p38 JNK CYLD IκB p50 p65 IκB NF-κB FLIP Bcl-X_L TNF TNFR2

Download TNF Receptor Signaling Pathway Map.

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.

Etanercept			Fas						99.20%
R-7050		CD40							98.56%
Oxazolone	TNFR1								≥98.0%
Utomilumab						4-1BB			99.33%
BIO8898		CD40L, IC₅₀: 25 μM							99.88%
TNF-α-IN-2		CD40, IC₅₀: 25 nM							98.75%
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							98.74%
Lucatumumab		CD40							98.18%
Toralizumab		CD40L							99.57%
GSK2245035		CD40, pEC₅₀: 6.5							99.85%
Ragifilimab								GITR
AQX-016A		CD40							98.00%
DRI-C25441		CD40, IC₅₀: 0.36 μM							99.53%
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

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TNF Receptor

TNF Receptor

TNF Receptor Isoform Specific Products:

TNF Receptor Isoform Specific Products:

TNF Receptor Related Products (545)

Recombinant Proteins (237)

Antibodies (23)

TNF Receptor Signaling Pathway

TNF Receptor Isoform Comparison

TNF Receptor Related Products (545):