NF-κB Activator

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.

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.

BAY-356, a potent TWEAK receptor agonist, is an aglycosylated anti-TWEAK receptor antibody. BAY-356 triggers TWEAKR hyperactivation, activates NFκB and STAT1 pathways, and undergoes TWEAKR-dependent internalization. BAY-356 can be used for the research of colorectal cancer, bladder cancer, non-small cell lung cancer and pancreatic cancer^[1][2].

MEDI-5083 is an Fc fusion protein that targets CD40 and is a CD40 agonist. MEDI-5083 stimulates CD40 signaling via NF-κB activation. MEDI-5083 upregulates MHCII, CD80, and CD86 expression, induces pro-inflammatory cytokine secretion, and enhances IFN-γ secretion by memory CD8⁺ T cells. MEDI-5083 can be used for the research of melanoma, colon carcinoma, and advanced solid tumors^[1][2].

TLR8 agonist 11 is a selective human Toll-like receptor 8 (TLR8) agonist. TLR8 agonist 11 activates the hTLR8-dependent NF-κB signaling pathway. TLR8 agonist 11 can be used for the research of inflammation and immune-related diseases.

Urocortin II, human TFA is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. Urocortin II, human TFA has an effect of promoting satiet and neuroprotective effect. Urocortin II, human TFA also has bactericidal, antiparasitic and pro-inflammation activity. Urocortin II, human TFA can activate NF-κB pathway and ERK1/2 MAP kinase. Urocortin II, human TFA can reduce pulmonary arterial hypertension and shows cardiac protection effect. Urocortin II, human TFA can be used for the researches of infection, inflammation, metabolic, neurological and cardiovascular disease.

NUCC-0227579 is a VHL-recruiting PROTAC degrader targeting CD73, with a DC₅₀ of 0.32 μM. NUCC-0227579 synergistically mediates CD73 degradation through the ubiquitin-proteasome pathway and the lysosomal pathway. NUCC-0227579 inhibits the conversion of AMP to adenosine, abrogates adenosine-mediated immunosuppression, upregulates the activities of the NF-κB and NFAT pathways, and enhances the secretion, activation and proliferation levels of IFN-γ and TNF-α. NUCC-0227579 downregulates NAD⁺ synthesis in tumor cells, and inhibits the proliferation, migration and adhesion abilities of tumor cells under glutamine-deficient conditions. NUCC-0227579 significantly suppresses tumor growth in a humanized NSG mouse model of triple-negative breast cancer.

Anti-inflammatory agent 107 is an orally active anti-inflammatory agent. Anti-inflammatory agent 107 inhibits and NF-κB with a superior binding affinity of -9.4578 kcal/mol. Anti-inflammatory agent 107 reduces levels of inflammatory biomarkers (TNF-α, IL-6, INF-γ, NF-κβ, C-reactive protein and Erythrocyte Sedimentation Rate) and enhances the endogenous antioxidant defense system by elevating SOD (Superoxide Dismutase), CAT (Catalase) and GSH (Glutathione) activities. Anti-inflammatory agent 107 not induces liver toxicity and demonstrates hepatoprotective effects. Anti-inflammatory agent 107 dose-dependently ameliorates leukocyte infiltration and tissue edema. Anti-inflammatory agent 107 can be used for anti-inflammatory research.

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.

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.

4-Hydroxybenzophenone-d₄ (4HBP-d₄) 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.

SHR-1806 is a OX40 agonist and a NF-κB activator, with antitumor activity. SHR-1806 mediates ADCC and CDC effects, enhances the function and expansion of effector T cells, suppresses regulatory T cells, and increases γ-interferon secretion. SHR-1806 exhibits typical pharmacokinetic characteristics and favorable safety profiles. SHR-1806 can be used in studies related to solid tumors and colon cancer.

LBL-019 is a humanized IgG1 monoclonal antibody targeting TNFR2. LBL-019 costimulates TNFR2 and activates the NF-κB signaling pathway in an Fc crosslinking-dependent manner. LBL-019 can be used for the research of advanced malignant tumors, including hepatocellular carcinoma and melanoma. The recommended isotype control is human IgG1 kappa (HY-P99001).

Centaurein, a flavonoid, is an IFN-γ promoter enhancer. Centaurein up-regulates the activity of NFAT and NF-κB enhancers. Centaurein increases the IFN-γ expression in T and NK cells and the serum IFN-γ level in mice. Centaureidin completely relaxes the contractions in intact rat aortic rings. Centaurein effectively protects mice against Listeria infection^[1][2][3][4].

Rhoifolin (Standard) is the analytical standard of Rhoifolin. This product is intended for research and analytical applications. Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines.