TNFRSF5/CD40
TNFRSF5/CD40 is a tumor necrosis factor receptor family member expressed by B cells, professional antigen-presenting cells, non-immune cells, and tumors[1]. Mechanistically, CD40-CD40L/CD154 engagement regulates humoral and cellular adaptive immunity, including B-cell proliferation, immunoglobulin isotype switching, and germinal center formation[1][2]. CD40 signaling recruits TRAFs and activates NF-κB, with additional involvement of PI3K/AKT, MAPKs, and JAK3/STAT pathways[3]. In inflammatory disease models, CD40 ligation promotes cytokines, chemokines, matrix metalloproteinases, growth factors, adhesion molecules, and procoagulant responses in vascular and immune-associated cells[4][5]. Compared with related pathway forms, CD40 and CD40L both have membrane and soluble forms, and soluble CD40 may bind CD40L and reduce transmembrane CD40 receptor activation[3][6]. For experimental applications, CD40 agonistic antibodies and CD40L-based strategies require receptor clustering or trimerization, while antagonistic approaches target autoimmune disease, allograft rejection, and inflammatory pathology[3][7].
References:
- [1]. Elgueta R, et al. Molecular mechanism and function of CD40/CD40L engagement in the immune system. Immunol Rev. 2009 May;229(1):152-72. [Content Brief]
- [2]. Lougaris V, et al. Hyper immunoglobulin M syndrome due to CD40 deficiency: clinical, molecular, and immunological features. Immunol Rev. 2005 Feb;203:48-66. [Content Brief]
- [3]. Tang T, et al. Molecular basis and therapeutic implications of CD40/CD40L immune checkpoint. Pharmacol Ther. 2021 Mar;219:107709. [Content Brief]
- [4]. Chatzigeorgiou A, et al. CD40/CD40L signaling and its implication in health and disease. Biofactors. 2009 Nov-Dec;35(6):474-83. [Content Brief]
- [5]. Schönbeck U, et al. CD40 signaling and plaque instability. Circ Res. 2001 Dec 7;89(12):1092-103. [Content Brief]
- [6]. Lakshman N, et al. Microglia in the spinal cord stem cell niche regulate neural precursor cell proliferation via soluble CD40 in response to myelin basic protein. Stem Cells. 2025 Feb 12;43(2):sxae076. [Content Brief]
- [7]. Richards DM, et al. Concepts for agonistic targeting of CD40 in immuno-oncology. Hum Vaccin Immunother. 2020;16(2):377-387. [Content Brief]
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TNFRSF5/CD40 Related Products (93)
Related Products (93)
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R-7050
0 ImagesSynonyms: TNF-α Antagonist IIIR-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
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(-)-Isoproterenol hydrochloride
0 ImagesSynonyms: Levisoprenaline hydrochloride; Proternol L hydrochloride(-)-Isoproterenol (Levisoprenalinel) hydrochloride is the R-isomer of Isoproterenol. (-)-Isoproterenol hydrochloride can reduce the cleavage of caspase 3 and TNFα levels in retinal endothelial cells (REC). (-)-Isoproterenol hydrochloride can be used for the study of diabetic retinopathy.
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Golimumab
0 ImagesSynonyms: CNTO-148Golimumab (CNTO-148) is a potent human IgG1 TNFα antagonist monoclonal antibody. Golimumab has anti-inflammation activitity and inhibits IL-6 and IL-1β production. Golimumab acts via targeting and neutralizing TNF to prevent inflammation and destruction of cartilage and bone. Golimumab has the anticancer activity and induces cell apoptosis. Golimumab can be used for rheumatoid arthritis, Crohn's disease and cancer research.
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BIO8898
0 ImagesCat. No.: HY-122663APurity: 98.08%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.
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TNF-α-IN-2
0 ImagesTNF-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.
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Usenamine A
0 ImagesCat. No.: HY-N20711CAS No.: 1428417-60-0Usenamine A is an orally active natural dibenzofuran compound with multiple biological activities such as anti-inflammatory and anticancer effects. Usenamine A inhibits the AKT/mTOR/STAT3/ID1 signaling axis and induces ubiquitin-proteasome degradation of ID1. Usenamine A targets the TNF-TNFR2 complex, inhibits RGS2, and interferes with Myosin-9/actin cytoskeleton remodeling. Usenamine A induces apoptosis, autophagy and ROS-mediated endoplasmic reticulum stress in cancer cells, inhibits cancer cell proliferation and invasion, and reduces the production of pro-inflammatory cytokines. Usenamine A alleviates arthritis-related symptoms. Usenamine A can be used in studies related to liver cancer, non-small cell lung cancer, rheumatoid arthritis and ankylosing spondylitis.
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JWX-A0108
0 ImagesCat. No.: HY-182707CAS No.: 2055045-42-4JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC50 of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease.
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COX-2/5-LOX-IN-8
0 ImagesCat. No.: HY-183764COX-2/5-LOX-IN-8 is an orally active dual COX-2/5-LOX inhibitor, with an IC50 of 6.30 μM against sheep-derived COX-2 and an IC50 of 8.09 μM against 5-LOX. COX-2/5-LOX-IN-8 acts as a membrane stabilizer that stabilizes erythrocyte membranes against hypotonicity-induced hemolysis. COX-2/5-LOX-IN-8 functions as a protein stabilizer that inhibits heat-induced denaturation of bovine serum albumin. COX-2/5-LOX-IN-8 reduces paw swelling, improves hind limb weight-bearing function, decreases serum levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, CRP), and lowers serum levels of cartilage degradation biomarkers (COMP, MMP-3, CTX-II). COX-2/5-LOX-IN-8 can be used in the research of osteoarthritis.
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Mitazalimab
0 ImagesSynonyms: ADC-1013; JNJ-64457107; VanalimabMitazalimab (ADC-1013; JNJ-64457107) is FcγR-dependent CD40 agonist with tumor-directed activity. Mitazalimab activates antigen-presenting cells, e.g. dendritic cells (DC), to initiate tumor-reactive T cells. Therefore, Mitazalimab induces tumor-specific T cells to infiltrate and kill tumors. Mitazalimab remodels the tumor-infiltrating myeloid microenvironment.
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UCB-5307
0 ImagesCat. No.: HY-147045CAS No.: 1515887-44-1UCB-5307 is a potent TNF signaling inhibitor with a KD of 9 nM for human TNFα. UCB-5307 can penetrate the preformed hTNF/hTNFR1 complex.
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Tegoprubart
0 ImagesSynonyms: AT-1501Tegoprubart (AT-1501) is a CD40 ligand inhibitor (EC50=100 ng/mL) and immunosuppressant that selectively inhibits the CD40 ligand, a co-stimulatory molecule involved in T cell activation. Tegoprubart suppresses immune rejection, prevents rejection in animal transplantation models, and reduces cell-mediated and antibody-mediated immune responses to create a more immunotolerant environment. Tegoprubart preserves renal function when combined with Mycophenolate (HY-B0421) and Corticosteroids, and maintains graft function in preclinical studies. Tegoprubart is applicable to research related to kidney transplantation and kidney transplant rejection.
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Carveol
0 ImagesCarveol is an orally active monoterpenoid alcohol with neuroprotective, antioxidant, anti-inflammatory, anticonvulsant, antidiabetic, hypolipidemic and hepatoprotective activities. Carveol upregulates the expression of Bcl2, downregulates the expression of caspase-3, TNF-α, IL1β and IL6, activates the Nrf2/HO-1 antioxidant signaling pathway, inhibits the RAGE/NF-κB signaling pathway, and suppresses neuroinflammation and neuronal apoptosis. Carveol inhibits α-synuclein aggregation, improves cognitive ability, and inhibits α-amylase activity. Carveol exerts neuroprotective effects in a rat model of Parkinson's disease. Carveol exhibits antidiabetic effects in alloxan-induced diabetic rats. Carveol alleviates PTZ-induced seizures in rats. Carveol can be used in research related to Parkinson's disease, epilepsy, diabetes and ischemic stroke.
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4-Methoxybenzyl alcohol
0 ImagesSynonyms: P-Methoxy-benzyl alcoho; (4-Methoxyphenyl)methanol4-Methoxybenzyl alcohol (P-Methoxy-benzyl alcoho; (4-Methoxyphenyl) methanol) is a naturally derived volatile aromatic compound. 4-Methoxybenzyl alcohol upregulates the phosphorylation level of PI3K/Akt pathway proteins, downregulates the expression of pro-inflammatory factors, increases the content of tight junction proteins occludin and claudin-5, and alleviates structural damage to the blood-brain barrier. 4-Methoxybenzyl alcohol improves the decrease in viability and NO level of cerebral microvascular endothelial cells induced by oxygen-glucose deprivation/reperfusion, and reduces the release of lactate dehydrogenase. 4-Methoxybenzyl alcohol serves as a substrate in the two-phase persulfate-mediated electro-oxidation system, where it is directionally oxidized to p-anisaldehyde. 4-Methoxybenzyl alcohol acts as a substrate for wild-type fungal aryl alcohol oxidase. 4-Methoxybenzyl alcohol can be used in studies related to ischemic stroke, as well as in research across various fields such as chemical synthesis, including the synthesis of fragrances and flavorings.
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TREM-1 inhibitory peptide GF9
0 ImagesSynonyms: Human TREM-1(213-221)TREM-1 inhibitory peptide GF9 (Human TREM-1 (213-221)) is a TREM-1 inhibitor. TREM-1 inhibitory peptide GF9 blocks the TREM-1 signaling pathway via a ligand-independent mechanism, spontaneously inserts into the cell membrane to dissociate TREM-1 from DAP-12, and functions through the Signaling Chain Homooligomerization (SCHOOL) model. TREM-1 inhibitory peptide GF9 reduces the levels of TNFα, IL-1β, IL-6, and M-CSF. TREM-1 inhibitory peptide GF9 inhibits tumor growth, prolongs the survival of mice with pancreatic cancer models, ameliorates collagen-induced arthritis, and exerts protective effects on bone and cartilage simultaneously. TREM-1 inhibitory peptide GF9 can be used in research related to arthritis, pancreatic cancer, retinopathy, alcoholic liver disease, and liver cancer.
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Toralizumab
0 ImagesSynonyms: IDEC-131; Anti-Human CD40 ligand Recombinant AntibodyToralizumab (IDEC-131) is a humanized monoclonal antibody (mAb) against CD40L (CD154) comprised of human gamma 1 heavy chains and human kappa light chains. Toralizumab binds specifically to human CD40L on T cells, thereby preventing CD40 signaling. Toralizumab is an immunosuppressive agent. Toralizumab can lead to increased thrombosis. Toralizumab can be studied in research for diseases such as multiple sclerosis, systemic lupus erythematosus (SLE), and Crohn’s disease.
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Edpetiline
0 ImagesEdpetiline is an anti-inflammatory agent. Edpetiline inhibits the phosphorylation of IκB, nuclear transcription/translocation of NF-κB p65, as well as the phosphorylation of p38 MAPK and ERK MAPK. Edpetiline reduces intracellular ROS levels, inhibits the expression of TNF-α, IL-6, iNOS, COX-2, and promotes the expression of IL-4. Edpetiline is applicable to the research of diseases associated with inflammation and oxidative stress.
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Lucatumumab
0 ImagesSynonyms: HCD122Lucatumumab (HCD122) is a fully human anti-CD40 antagonist monoclonal antibody, which blocks CD40/CD40L-mediated signaling. Lucatumumab efficiently mediates antibody-dependent cell-mediated cytotoxicity (ADCC) and clearance of tumor cells, can be used for refractory lymphomas, CLL and multiple myeloma research.
