TNF Receptor Inhibitor

Geniposidic acid is an orally active FXR modulator and SIRT6 activator. Geniposidic acid binds to the Ser332 and His447 sites on the FXR ligand-binding domain, thereby driving nuclear translocation, coactivator recruitment, and transcription of downstream bile acid and cholesterol metabolism-related genes. Geniposidic acid improves metabolic dysfunction-related fatty liver disease by activating the SIRT6 signaling pathway. Geniposidic acid inhibits inflammation and modulates gut microbiota to alleviate colitis. Geniposidic acid can be used in research on drug-induced liver injury, inflammatory bowel disease, metabolic dysfunction-related fatty liver disease, and metabolic dysfunction-related steatohepatitis.

Anti-Mouse TNF alpha Antibody (TN3-19.12) is an anti-mouse TNF alpha IgG antibody inhibitor derived from host Armenian Hamster. Anti-Mouse TNF alpha Antibody (TN3-19.12) neutralizes cytotoxic activity in supernatants obtained from LNC-8 cells. Anti-Mouse TNF alpha Antibody (TN3-19.12) reduces the symptoms and severity of EAE (experimental allergic encephalomyelitis) in LNC-8 cells xenograft mice models. Anti-Mouse TNF alpha Antibody (TN3-19.12) prevents diabetes in NOD mice. Anti-Mouse TNF alpha Antibody (TN3-19.12) shows apparent radiosensitizing effect in CD2F1 mice.

Terameprocol is an inhibitor targeting the Sp1 transcription factor, which can selectively inhibit the transcription of Sp1-dependent genes. Terameprocol exerts its effects by inhibiting Sp1-mediated gene transcription, such as reducing the expression of genes like CDC2, survivin and HMGB1, thereby arresting the cell cycle, inducing apoptosis, and suppressing the inflammatory response. Terameprocol exhibits anti-proliferative, pro-apoptotic, and anti-inflammatory activities and is currently mainly used in the research of diseases such as cancer and pulmonary arterial hypertension[1][2][3].

Curcumenol ((+)-Curcumenol) is a natural compound with oral efficacy, exhibiting an IC₅₀ of 12.6 μM and a K_i of 10.8 μM against human CYP3A4. Curcumenol inhibits TNFα-induced phosphorylation/degradation of IκBα, phosphorylation/nuclear translocation of NF-κB p65, as well as the upregulation of MMP3, MMP9, MMP13, TRAF3, IL1RL1, TNFα and IL-1β. Curcumenol suppresses LPS-induced phosphorylation of Akt and p38 MAPK, as well as the production of pro-inflammatory mediators/proteins, and downregulates the SLC7A11/NF-κB/TGF-β pathway. Curcumenol binds to and inhibits the activation of Fyn and Lyn, blocks the function of downstream FcεRI signaling components, and reduces the release of allergic mediators/cytokines. Curcumenol upregulates the expression of KDM6B, and promotes chondrocyte proliferation and cartilage repair. Curcumenol induces ferroptosis and apoptosis, regulates the EMT process, and inhibits tumor growth and metastasis of triple-negative breast cancer. Curcumenol possesses anti-inflammatory, neuroprotective, antioxidant, antitumor, antiviral and hepatoprotective activities. Curcumenol can be used in research related to intervertebral disc degeneration, cancer, inflammation, central nervous system neurodegenerative diseases, allergic reactions and knee osteoarthritis.

Pexmetinib (ARRY-614) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis.

Tiratricol is an orally available thyroid hormone analog that inhibits pituitary thyroid-stimulating hormone secretion. Tiratricol is an intracellular toxin neutralizer that inhibits LPS and lipid A cytotoxicity with IC₅₀s of 20 μM and 32 μM, respectively. Tiratricol reduces TNF production in lipopolysaccharide-stimulated macrophages. Tiratricol also has antiviral activity and is an inhibitor of yellow fever virus (Flavivirus). It can bind to the RdRp domain of the viral NS5 protein to hinder YFV replication..

Anti-Mouse CD40 Antibody (FGK4.5/FGK45) is an agonistic rat-derived IgG2a monoclonal antibody targeting mouse CD40. Anti-Mouse CD40 Antibody (FGK4.5/FGK45) enhances T cells responses, dendritic cells maturation and NK cells activation. Anti-Mouse CD40 Antibody (FGK4.5/FGK45) can be used for the researches of cancer, infection, inflammation and immunology, such as CT26 tumor, vesicular stomatitis virus (VSV) infection and transplantation.

Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptor_A (GABA_A)-mediated ion channel currents (I_GABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.

TNF-α-IN-6 (compound 12) is an orally effective allosteric inhibitor of TNFα (K_D = 6.8 nM). TNF-α-IN-6 has anti-inflammatory effects.

Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma.

UCB-6876 is a TNFα inhibitor. UCB-6876 specifically binds to the asymmetric crystalline form of TNF-α trimer with a K_D of 22 μM. UCB-6876 is applicable to research related to autoimmune diseases (rheumatoid arthritis and Crohn's disease).

Peimine (Verticine; Dihydroisoimperialine) is an orally active natural product. Peimine has anti-inflammatory, analgesic and cough relieving effects. Peimine can be used in cancer and inflammation related research.

Atrosimab is an Fv-Fc1K fusion protein with an EC₅₀ value of 0.37 nM against humans. Atrosimab inhibits TNF-induced TNFR1 activation, release of IL-6 and IL-8, and cell death, and alleviates neuroinflammation. Atrosimab is applicable to research related to inflammatory diseases, neurodegenerative diseases, acute and chronic inflammation, experimental arthritis, non-alcoholic steatohepatitis, and experimental autoimmune encephalomyelitis.

Lysozyme (Muramidase) is a conserved antimicrobial protein. Lysozyme exerts its bactericidal effect by hydrolyzing bacterial cell wall peptidoglycan (PG). Lysozyme plays an important role in limiting bacterial growth on mucosal surfaces and other sites, not only controlling potential pathogens but also limiting overgrowth of microbiota to prevent dysbiosis. Extracellular lysozyme can also degrade polymeric PG into soluble fragments, activate NOD receptors in mucosal epithelial cells, and lead to the secretion of chemokines and activating factors by neutrophils and macrophages.

Lenalidomide hemihydrate (CC-5013 hemihydrate) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide hemihydrate induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide hemihydrate promotes IL-2 release and effector functions of CD8⁺ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide hemihydrate can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.

STAT1/3-IN-1 is a potent STAT1/3 inhibitor with potent anti-inflammatory effect. STAT1/3-IN-1 inhibits phosphorylation and nuclear translocation of STAT1/3 to modulate microglial inflammation, reduces LPS (HY-D1056)-induced pro-inflammatory cytokines (NO, IL-1β, IL-6, and TNF-α) and inflammatory mediators (iNOS, COX-2). STAT1/3-IN-1 exhibits low toxicity in mice. STAT1/3-IN-1 can be used for the research of neuroinflammation.

Tabalumab (LY2127399) is a human anti-BAFF (B-cell activating factor) monoclonal antibody (IgG4 type) with neutralising activity against membrane bound and soluble BAFF. Tabalumab can be used in studies of autoimmune diseases such as rheumatoid arthritis, renal failure and systemic lupus erythematosus.

10-Hydroxy-2-decenoic acid (10-HDA) is an orally active unsaturated medium-chain fatty acid with various physiological activities. 10-Hydroxy-2-decenoic acid induces ROS-mediated apoptosis in A549 cells. 10-Hydroxy-2-decenoic acid inhibits VEGF-induced angiogenesis in human venous endothelial cells. 10-Hydroxy-2-decenoic acid alleviates non-alcoholic fatty liver disease (NAFLD) by activating the AMPK-α signaling pathway. 10-Hydroxy-2-decenoic acid protects against bone loss by inhibiting NF-κB signaling downstream of FFAR4. 10-Hydroxy-2-decenoic acid is an antibiotic against many bacteria and fungi, such as Neurospora sitophila, molds and Staphylococcus aureus. 10-Hydroxy-2-decenoic acid has longevity-promoting effects in C. elegans. 10-Hydroxy-2-decenoic acid prevents osteoarthritis by targeting aspartyl β hydroxylase and inhibiting chondrocyte senescence.

Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC₅₀ of 53.6 μM.

Loganin is a type of iridoid glycoside compound that possesses anti-inflammatory, antioxidant, and antitumor properties, and offers protective effects against acute lung injury and pulmonary fibrosis. Loganin exerts its protective effects against LPS (HY-D1056)-mediated inflammation and oxidative stress by upregulating the Nrf2/HO-1 signaling pathway, and it reduces neuroinflammation caused by spinal cord injury (SCI).