TNF Receptor Activator

TNF-α (31-45), human TFA is a potent NF-kB pathway activator. TNF-αis a proinflammatory cytokine that induces necrosis or apoptosis. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis.

Arecaidine hydrochloride is a GABA transport system inhibitor. Arecaidine hydrochloride inhibits the proliferation of oral mucosal fibroblasts, increases the secretion of IL-6, TGF-β and TNF-α in cells, downregulates the expression of PPAR-γ and PCK1 in cells, and upregulates the expression of TGF-β1. Arecaidine hydrochloride inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine hydrochloride inhibits hPAT1-mediated L-[³H]proline uptake in cells. Arecaidine hydrochloride can be used in research related to neurological diseases.

γ-Hexalactone (γ-Caprolactone) is a gamma-lactone found in ripe fruits. γ-Hexalactone induces DNA damage in human lymphocytes and HepG2 cells, modulates cytokine secretion in human lymphocytes, and reduces recombinant PON1 activity. γ-Hexalactone serves as a dose-dependent oviposition inhibitor against Bactrocera oleae. γ-Hexalactone can be used for the research of Bactrocera oleae pest management.

Defensin HNP-1 human TFA is a type of human neutrophil peptide (HNPs). Defensin HNP-1 human TFA possesses immunomodulatory functions and can delay the apoptosis of neutrophils. Defensin HNP-1 human TFA inhibits DNA/RNA/protein synthesis and interferes with metabolic pathways, thus exhibiting broad antibacterial activity. Defensin HNP-1 human TFA has direct inactivation effects on HIV, HSV-1, HSV-2, CMV, influenza virus, etc. Defensin HNP-1 human TFA has antileishmanial activity. Defensin HNP-1 human TFA is involved in endothelial cell dysfunction during the early development of atherosclerosis.

RP-182 is a synthetic immunomodulatory peptide that exerts anti-tumor effects by targeting the mannose receptor CD206 (K_d = 8 μM) on the surface of tumor-associated macrophages (TAMs). RP-182 induces a conformational switch of the CD206 receptor, which activates NF-κB signaling and phagocytosis in CD206^high TAMs. RP-182 has dual function: activation of canonical NF-κB signaling, triggering TNFα secretion and autocrine activation of the TNF receptor 1 (TNFR1), leading to activation of caspase 8, apoptosis, and cell death. RP-182 is used in pancreatic cancer and melanoma research.

RP-832c is a synthetic analogue of host defense peptides (HDP), targeting the mannose receptor CD206 on the surface of M2 polarized macrophages (K_d = 3.5 μM). RP-832c binding to CD206 induces a significant conformational change in the receptor, activating signaling pathways that lead to rapid apoptosis and repolarization of CD206-positive M2 macrophages to an M1 phenotype. RP-832c treatment significantly reduces CD206 gene expression in M2 macrophages while transiently increasing expression of TNF-α, a marker for M1 macrophages. RP-832c is used for the studies of T-cell lymphoma (CTCL) and idiopathic pulmonary fibrosis (IPF).

HDMAPP triammonium is a potent phosphoantigen in the ammonium form and the pyrophosphate form of (E)-HDMAPP. HDMAPP is also a potent activator of γδ T cells and can induce T cell stimulation in vitro (EC₅₀=0.39 nM, TNF-α).

Tris(2-chloroethyl)phosphate-d₁₂ is the deuterium labeled Tris(β-chloroethyl) phosphate. Tris(2-chloroethyl) phosphate is a widely used organic phosphorus flame retardant, mainly used as a plasticizer. Tris(2-chloroethyl) phosphate has orally active hepatotoxicity, inducing an increase in reactive oxygen species (ROS) and calcium ions (Ca²⁺) influx, a decrease in mitochondrial membrane potential (△Ψm), and causing DNA damage and cell apoptosis. Tris(2-chloroethyl) phosphate directly binds to FXR, inducing obesity and the formation of fatty liver in mice. Chloroethyl) phosphate activates the TLR4/NF-κB pathway, triggering liver inflammation.

Calotatug ginistinag (XMT-2056) is an antibody-drug conjugate (ADC) targeting HER2, linked to a payload composed of XMT-1519 conjugate-1 (HY-148067) and STING agonist-20 (HY-148068). Calotatug ginistinag activates the STING signaling pathway in tumor cells and tumor-resident immune cells, induces the production of type I interferons and cytokines (CXCL10, IFN-β, IL-6, TNF-α, triggers innate anti-tumor immune responses, and exerts a bystander effect. Calotatug ginistinag exhibits efficacy against HER2-expressing cancer cells in co-culture with PBMCs. Calotatug ginistinag induces tumor regression and reduces systemic inflammation in various tumor models. Combination treatment with Calotatug ginistinag, Trastuzumab (HY-P9907) and T-DXd (HY-138298) yields benefits. Calotatug ginistinag can be used in studies related to HER2-expressing solid tumors such as breast cancer, gastric cancer and ovarian cancer.

Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (K_d=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC₅₀s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo.

GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC₅₀s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma.

M199 is a potent TLR3/TLR9 signaling inhibitor. M199 induces secretion of IL-6, IL-8 and TNFα in human PBMCs. M199 is used as a selective inducer of the immune response.

Anti-Mouse TREM2 Antibody (178) is an antibody targeting mouse TREM2, which blocks the binding of ligands to TREM2 and inhibits TREM2-mediated signaling pathways. Anti-Mouse TREM2 Antibody (178) inhibits the tumor growth of MCA/1956 sarcoma in mice. Anti-Mouse TREM2 Antibody (178) enhances IFNγ production by intratumoral CD8⁺ T cells and TNFα production by intratumoral CD4⁺ T cells. Anti-Mouse TREM2 Antibody (178) can be used in the research of sarcoma, colorectal cancer and breast tumors. The recommended isotype control is Rat IgG2a kappa, Isotype Control (HY-P990679).

BI-1910 is an agonistic human IgG2 monoclonal antibody targeting TNFR2, which selectively binds to human TNFR2 without inhibiting TNF-α binding. As an endogenous agonist, BI-1910 activates TNFR2 and mediates the activation of the NF-κB signaling pathway. Its agonistic activity is independent of FcγR or cross-linking; it can directly costimulate T cells and NK cells, induce T cell proliferation, and activate tumor-specific CD8+ T cells. BI-1910 exhibits antitumor activity in vivo, and shows an additive antitumor effect when combined with anti-PD-1 (HY-P9902). It can be used in research related to advanced/metastatic non-small cell lung cancer and hepatocellular carcinoma. Recommended isotype control: Human IgG2 lambda, Isotype Control (HY-P991206).

Arecaidine hydrobromide is a GABA transport system inhibitor. Arecaidine hydrobromide inhibits the proliferation of oral mucosal fibroblasts, increases the secretion of IL-6, TGF-β and TNF-α in cells, downregulates the expression of PPAR-γ and PCK1 in cells, and upregulates the expression of TGF-β1. Arecaidine hydrobromide inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine hydrobromide inhibits hPAT1-mediated L-[³H]proline uptake in cells. Arecaidine hydrobromide can be used in research related to neurological diseases.

TLR7 agonist 4 is a TLR7 agonist with pro-inflammatory cytokine-stimulating activity. TLR7 agonist 4 modulates TLR7 activity to stimulate the production of pro-inflammatory cytokines. TLR7 agonist 4 stimulates mouse bone marrow-derived macrophages to produce the pro-inflammatory cytokine TNFα. TLR7 agonist 4 can be conjugated with antibodies to form conjugates. TLR7 agonist 4 is applicable to cancer research.

Phoxim is an organophosphorus pesticide and an orally active inhibitor of cholinesterase and CYP3A, which induces neurotoxicity in Caenorhabditis elegans and causes nephrotoxicity characterized by glomerular atrophy and interstitial fibrosis. Phoxim induces inhibition of the autophagy pathway. Phoxim induces dopaminergic neuron degeneration and exacerbates Aβ-induced paralysis. Phoxim damages enterocytes and disrupts intestinal barrier integrity. Phoxim induces ROS accumulation. Phoxim induces mitochondrial apoptosis, involving upregulation of Bad, Bax, caspase-3, and caspase-9 and downregulation of Bcl-2. Phoxim inhibits mitochondrial functional enzymes (COX, Ca²⁺-Mg²⁺-ATPase, SDH). Phoxim upregulates Nrf2 mRNA expression in the jejunal mucosa. Phoxim increases TNF-α and decreases IL-6 and IL-8 in the intestinal mucosa. Phoxim alters gut microbial composition by increasing total bacteria and Escherichia coli and reducing Lactobacillus. Phoxim enhances energy metabolism in silver carp by upregulating key glycolytic and gluconeogenic enzymes. Phoxim is used in research on neurodegenerative diseases, nephrotoxicity, intestinal oxidative stress and barrier dysfunction, and bacterial sepsis.

RP-182 acetate is a synthetic immunomodulatory peptide that exerts anti-tumor effects by targeting the mannose receptor CD206 (K_d = 8 μM) on the surface of tumor-associated macrophages (TAMs). RP-182 acetate induces a conformational switch of the CD206 receptor, which activates NF-κB signaling and phagocytosis in CD206^high TAMs. RP-182 acetate has dual function: activation of canonical NF-κB signaling, triggering TNFα secretion and autocrine activation of the TNF receptor 1 (TNFR1), leading to activation of caspase 8, apoptosis, and cell death. RP-182 acetate is used in pancreatic cancer and melanoma research.

SMU-Z1 is a TLR1/2 heterodimer agonist with an EC₅₀ of 4.88 nM. SMU-Z1 activates the NF-κB pathway, triggers pro-inflammatory cytokine production, and induces the generation of TNF-α, IL-1β, IL-6 and NO. SMU-Z1 promotes splenocyte proliferation and upregulates the expression of CD8⁺T cells, NK cells and dendritic cells. SMU-Z1 exhibits significant anti-tumor effects in mouse leukemia models. SMU-Z1 can be used for leukemia-related research.

Anti-CD160 Antibody (MAT 302) (CL1-R2) is a human monoclonal antibody targeting CD160. Anti-CD160 Antibody (MAT 302) blocks the CD160-HVEM protein interaction, inhibits FGF2-mediated renal tubular vascular growth, and induces endothelial cell apoptosis. Anti-CD160 Antibody (MAT 302) targets CD160 on neovascularization to exert anti-angiogenic and vascular normalization effects, trigger the production of IFN-γ, TNF and IL-6 by NK cells, and enhance glucose metabolism of NK cells through the AKT/mTOR/s6k signaling pathway. Anti-CD160 Antibody (MAT 302) reduces vascular density, normalizes remaining tumor blood vessels, and inhibits tumor growth in melanoma-bearing mice. Anti-CD160 Antibody (MAT 302) can be used in research related to neovascularization, proliferative diabetic retinopathy, and melanoma.