NF-κB Activator

1Z105 is an orally active TLR4/MD2 agonist, immunostimulant and vaccine adjuvant. 1Z105 activates NF-κB via the MyD88/TRIF pathway in a CD14-independent manner, with EC₅₀ values of 0.63 µM and 0.77 µM for inducing IL-6 and IL-12 in mBMDCs, respectively. 1Z105 promotes dendritic cell maturation, antigen uptake and cross-presentation; when used alone, it induces Th2-IgG1, while combined with the TLR7 agonist 1V270, it synergistically induces balanced Th1/Th2 responses and provides low-reactogenic protection against homologous, heterologous and heterosubtypic influenza. 1Z105 prevents LPS (HY-D1056A1)- and galactosamine-induced liver injury as well as autoantibody-driven arthritis in mice. 1Z105 can be used in studies related to influenza virus infection, inflammation, and LPS/galactosamine-induced liver injury.

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.

HSV-60mer sodium is a 60 bp double-stranded DNA oligonucleotide derived from the HSV-1 genome, and also an IFNβ inducer. HSV-60mer sodium colocalizes with endogenous cytoplasmic IFI16 in immune cells. HSV-60mer sodium activates the transcription factors IRF3 and NF-κB, induces the production of proinflammatory cytokines, and inhibits HSV-1 replication in immune cells. HSV-60mer sodium can be used in studies related to herpes simplex virus type 1 infection.

Methylchloroisothiazolinone is a widely used fungicide and also an aquatic pollutant with pro-inflammatory activity and neurotoxicity. Methylchloroisothiazolinone induces the production of pro-inflammatory cytokines (such as IL-1β, TNF-α, IL-6) by activating the NF-κB signaling pathway and upregulating TLR4 expression, thereby triggering allergic contact dermatitis. Methylchloroisothiazolinone reduces cholinesterase activity and exacerbates oxidative stress by impairing catalase activity and disrupting redox balance. Methylchloroisothiazolinone poses significant harm to Mediterranean mussels, reducing the viability of hemocytes and digestive gland cells, inhibiting immune phagocytic function, and disrupting osmoregulatory capacity. Methylchloroisothiazolinone is used in studies on allergic contact dermatitis and related immunotoxicity mechanisms.

Fluopyram (Standard) is the analytical standard of Fluopyram (HY-119459). This product is intended for research and analytical applications. Fluopyram is an orally active succinate dehydrogenase inhibitor, antifungal and nematicide. Fluopyram inhibits succinate dehydrogenase activity, activates CAR/PXR nuclear receptors, and increases caspase-3, TNF-α and NF-κB. Fluopyram inhibits the growth of F. virguliforme, Botrytis cinerea and Alternaria solani with EC₅₀ values of 3.35, 5.389 and 0.244 µg/mL, respectively. Fluopyram induces liver and thyroid tumor formation. Fluopyram is nephrotoxic and embryotoxic.

4-Hydroxybenzophenone-d₅ (4HBP-d₅) is the deuterated-labeled 4-Hydroxybenzophenone (HY-W014937). 4‑Hydroxybenzophenone (4HBP) is a major metabolite of Benzophenone (HY-Y0546) and is orally active. 4-Hydroxybenzophenone triggers endoplasmic reticulum stress and activates the PERK-eIF2α-ATF4-CHOP and IRE1α-XBP1s pathways, and inhibits IκB translation. 4-Hydroxybenzophenone induces endoplasmic reticulum stress, unfolded protein response activation, protein homeostasis imbalance, protein aggregation, oxidative stress, ROS accumulation, mitochondrial membrane potential decrease, ATP depletion, and cytotoxicity. 4-Hydroxybenzophenone induces neural stem cell apoptosis (apoptosis) and affects neuronal differentiation. 4-Hydroxybenzophenone promotes malignant proliferation of hepatocellular carcinoma cells and xenograft tumor growth in nude mice. 4-Hydroxybenzophenone can be used in research related to neurodevelopmental toxicity and hepatocellular carcinoma.

DpC hydrochloride is a selective, orally active iron chelator with anticancer activity. DpC hydrochloride acts on signaling pathway-related targets such as JNK, NF-κB, and its activity is competitively inhibited by another iron chelator Dp44mT (HY-18973). By chelating intracellular iron and copper ions in tumor cells to form redox-active complexes, DpC hydrochloride induces oxidative stress, activates the JNK, NF-κB pathways and downregulates IκBα, upregulates the expressions of neuroglobin and cytoglobin, activates caspase 3/9 to induce tumor cell apoptosis. It also overcomes P-glycoprotein-mediated multidrug resistance through a lysosome-targeting mechanism, and exhibits broad-spectrum synergistic effects when combined with various chemotherapeutic agents. DpC hydrochloride inhibits tumor metastasis and increases TNF-α levels in the tumor microenvironment to enhance endogenous immune responses. DpC hydrochloride is applicable to the research of various malignancies including neuroblastoma, pancreatic cancer, prostate cancer, lung cancer, and breast cancer.

Penehyclidine, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation.

MG-1131 is a human monoclonal antibody (mAb) targeting TIGIT. MG-1131 activates NF-κB signaling in T cells and enhances NK-mediated tumor killing activity in a PVR-dependent manner. MG-1131 blocks TIGIT to increase IFN-γ secretion. MG-1131 can be used in anti-tumor immunity research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).

Pellitorine (Standard) is the analytical standard of Pellitorine (HY-N3097). Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria.

Apoptosis/necroptosis inducer 1 is an orally active and brain-penetrant apoptosis and necroptosis inducer. Apoptosis/necroptosis inducer 1 induces mitochondria-dependent (intrinsic pathway) apoptosis. Apoptosis/necroptosis inducer 1 induces necroptosis by activating the TNF-α/NF-κB/MAPK signaling pathway. Apoptosis/necroptosis inducer 1 exhibits antiproliferative activity in glioblastoma cell lines and multiple solid tumor types. Apoptosis/necroptosis inducer 1 inhibits growth of orthotopic glioblastoma in animal models and improves survival rate. Apoptosis/necroptosis inducer 1 can be used for the research of glioblastoma.

iE-DAP is a Nod1 agonist. iE-DAP activates NOD1, which in turn activates the NF-κB signaling pathway and MLCK signaling pathway, inducing cellular inflammatory responses and tight junction disruption. iE-DAP downregulates the expression of ZO-1 and Occludin genes. iE-DAP increases the secretion of IL-6, GRO-α, MCP-1, IL-8 and MIP-1β in term human trophoblast cell cultures. iE-DAP triggers preterm birth in pregnant mice, reduces fetal body weight, and induces fetal inflammation. iE-DAP is applicable to research related to mastitis and preterm birth.

Nrf2 activator-23 is an orally active Keap1 binder and Nrf2 activator, with K_D values of 28.68 nM and 54.55 nM for Keap1 and its Kelch domain, respectively. Nrf2 activator-23 disrupts the Keap1-Nrf2 interaction, reduces ubiquitination and degradation of Nrf2, and activates the Nrf2 signaling pathway. Nrf2 activator-23 inhibits RANKL-induced osteoclast formation, bone resorptive activity, ROS production, and activation of the MAPK and NF-κB signaling pathways, while downregulating the expression of osteoclast-specific genes and proteins. Nrf2 activator-23 attenuates bone loss and reduces osteoclast formation in vivo without affecting osteoblast differentiation and mineralization. Nrf2 activator-23 can be used for the research of osteoporosis.

H1L1A1B3 is an ionizable cationic lipid used in the formation of lipid nanoparticles (LNPs) for the delivery of circular RNA (circRNA). H1L1A1B3-LNPs demonstrates a fourfold increase in circRNA transfection efficiency in lung cancer cells over ALC-0315 (HY-138170). H1L1A1B3 can activate the NF-κB/IRF immune pathways.

SMU-C68 is a highly selective small-molecule TLR1/2 heterodimer agonist (EC₅₀=0.009 μM). SMU-C68 activates NF-κB and MAPK pathways to promote pro-inflammatory cytokine release (e.g., TNF-α, IL-1β). SMU-C68 is promising for research of cancers.

Anabsinthin is a dimeric sesquiterpene lactone. Anabsinthin can be found in Artemisia absinthium L. (wormwood). Anabsinthin modulates intracellular calcium levels, mediates anti-inflammatory and antioxidant effects. Anabsinthin inhibits Phorbol 12-myristate 13-acetate (HY-18739)-induced superoxide anion production, increased iNOS and MUC5AC protein expression, and IL-1β transcription upregulation. Anabsinthin can be used for the research of citrus canker.

PE0116 is a fully human CD137 agonistic monoclonal antibody generated from immunized harbor H2L2 human transgenic mice. PE0116 is a ligand block. PE0116 activates NF-κB signaling which significantly promotes T-cell proliferation and increases cytokine secretion in vitro. PE0116 exhibits robust antitumor activity in MC38 tumor model.

Potassium dihydrogen phosphate, United States Pharmacopeia (USP) Reference Standard (Potassium phosphate monobasic (Pharmaceutical primary standard, USP)) is a potassium salt. Potassium dihydrogen phosphate, United States Pharmacopeia (USP) Reference Standard activates NF-κB. Potassium dihydrogen phosphate, United States Pharmacopeia (USP) Reference Standard upregulates the expression of dental/osteogenic markers (OCN, DSP/DSPP, OSX, RUNX2, ALP) and enhances the mineralization capacity of human periodontal ligament stem cells. Potassium dihydrogen phosphate, United States Pharmacopeia (USP) Reference Standard promotes the proliferation of human periodontal ligament stem cells in logarithmic growth phase. Potassium dihydrogen phosphate, United States Pharmacopeia (USP) Reference Standard promotes the growth of somatic embryos of Dendrobium Sonia, increases leaf number, leaf length and fresh weight of tissue-cultured seedlings. Potassium dihydrogen phosphate, United States Pharmacopeia (USP) Reference Standard is applicable to periodontal disease-related research.

Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis.

GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer.