TNF Receptor Activator

Tris(2-chloroethyl) phosphate (TCEP) 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.

CRAMP (mouse) is an antibacterial peptide and a functional homolog of LL-37. CRAMP (mouse) exhibits potent antibacterial activity against Gram-negative bacteria. The complex formed by CRAMP (mouse) and CpG can activate macrophages to secrete TNF-α. CRAMP (mouse) plays a key role in wound healing, immune regulation and maintenance of intestinal homeostasis.

β-Eudesmol has anticancer and anti-inflammatory activities. Beta-Eudesmol can induce apoptosis. β-Eudesmol is a neostigmine antagonist. β-Eudesmol can antagonize neostigmine-induced neuromuscular failure. β-Eudesmoll can be used in the study of sepsis diseases. β-Eudesmol is a sesquiterpene-like compound that can be extracted from the rhizome of Atractylodes lancea.

Bioymifi (DR5 Activator), a potent TRAIL receptor DR5 activator, binds to the extracellular domain (ECD) of DR5 with a K_d of 1.2 μM. Bioymifi can act as a single agent to induce DR5 clustering and aggregation, leading to apoptosis.

ODN M362 sodium is a TLR9 agonist that acts as a vaccine adjuvant. ODN M362 sodium activates mouse splenocytes, induces apoptosis in human hepatocellular carcinoma cells, upregulates proinflammatory cytokines in human hepatocellular carcinoma cells, and inhibits the proliferation of human hepatocellular carcinoma cells. ODN M362 sodium upregulates the expression of TLR9/TLR6, activates downstream signaling pathways via IRAK4 and IRF7, and strongly amplifies antigen-specific cellular immune responses to participate in innate immune activation. ODN M362 sodium can be used in research related to hepatocellular carcinoma and breast cancer.

Thiophanate-Methyl is a pesticide residue and fungicide. Thiophanate-Methyl induces hepatotoxicity via caspase-3-mediated apoptosis and oxidative stress, thereby causing metabolic imbalance in the liver of zebrafish. Thiophanate-Methyl impairs the rhizobacteria-mediated defense response of cucumber against fusarium wilt.

Fluorene is an orally active polycyclic aromatic hydrocarbon (PAH) and a precursor to other fluorene-based compounds. Fluorene and its derivatives serve as dye precursors for fluorene synthesis. In A549 cells, Fluorene induces oxidative stress and inflammatory responses by increasing ROS and SOD generation, exacerbating lipid peroxidation, modulating antioxidant enzyme activity, and upregulating the expression of pro-inflammatory factors TNF-α and IL-6. In vivo, Fluorene exhibits anxiolytic activity. Fluorene holds potential for research in inflammation and neurological disorders.

Kaolin is a family of kaolinitic clays, which is found in the earth's crust. Kaolin alleviates the toxicity of graphene oxide for mammalian cells. Kaolin can be utilized in industrial, cosmetic and medical fields, excipient.

NGM-438 is a humanized monoclonal antibody antagonist of LAIR1, with a K_a of 0.26 nM for human LAIR1 and 4.28 nM for cynomolgus monkey LAIR1. NGM-438 blocks the binding of LAIR1 to its Collagen ligand and antagonizes the Collagen-induced LAIR1 signaling pathway. NGM-438 reverses FcγR signaling inhibition in myeloid cells, induces dendritic cells to secrete TNFα, promotes T cell proliferation, and triggers myeloid inflammation and allogeneic T cell responses. NGM-438 sensitizes refractory mouse lung cancer to PD-1 blockade, increases the content of intratumoral CD8⁺ T cells and the expression of inflammatory genes. NGM-438 is applicable to research related to solid tumors, refractory solid tumors and non-small cell lung cancer.

Arecaidine is a GABA transport system inhibitor. Arecaidine 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 inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine inhibits hPAT1-mediated L-[³H]proline uptake in cells. Arecaidine can be used in research related to neurological diseases.

MG-T-19 is a potent small-molecule inhibitor targeting human TIM-3. MG-T-19 blocks the interactions between TIM-3 and its ligands such as phosphatidylserine, CEACAM1 and Galectin-9. MG-T-19 promotes the secretion of TNF-α and IFN-γ by peripheral blood mononuclear cells, and significantly enhances their ability to inhibit cancer cell proliferation. MG-T-19 can be used in studies related to acute myeloid leukemia.

LY 303511 hydrochloride is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K⁺ currents (IC₅₀=64.6±9.1 μM) in MIN6 insulinoma cells.

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).

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.

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.

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.

MB-314 is a human IgG1 monoclonal antibody (mAb) targeting Lewis Y. MB-314 induces enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. MB-314 increases the release of IFN-γ, TNF-α, MCP-1, and IL-6. MB-314 can be used in cancer research.

SMU-C409 is a TLR1/2 agonist with an EC₅₀ of 65 nM in HEK-Blue hTLR2 Cells. SMU-C409 activates the TLR1/2–MyD88–NF-κB pathway, inducing TNF-α/IL-1β secretion and robust immune cell activation for antitumor immunomodulation. SMU-C409 shows low toxicity in virto. SMU-C409 can be used for cancer immunotherapy research.

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.