TNF Receptor Inhibitor

Vulgarin is an orally active, naturally occurring eudesmane sesquiterpene with multiple biological activities including anti-inflammatory and antioxidant properties. Vulgarin targets and inhibits HMGB1, NF-κB and iNOS, while regulating key genes involved in hepatic gluconeogenesis; it also blocks inflammatory signaling pathways and inhibits the production and release of pro-inflammatory cytokines such as TNF-α and IL-1β. Vulgarin effectively alleviates pancreatic oxidative stress by reducing lipid peroxidation levels and restoring antioxidant enzyme activity. Vulgarin reverses abnormally elevated serum pancreatic enzyme levels, preserves the integrity of pancreatic acinar cells, and reduces pancreatic edema, hemorrhage and inflammatory infiltration. Vulgarin remodels the function of pancreatic endocrine cells, restores insulin content in β cells, and downregulates glucagon levels in α cells and somatostatin levels in δ cells. Vulgarin can be used in studies related to pancreatic injury and diabetes.

2-(2,6-Dioxopiperidin-3-yl)phthalimidine (Standard) is the analytical standard of 2-(2,6-Dioxopiperidin-3-yl)phthalimidine. This product is intended for research and analytical applications. 2-(2,6-Dioxopiperidin-3-yl)phthalimidine (EM-12), a teratogenic Thalidomide analogue, is more active than Thalidomide and is much more stable for hydrolysis. 2-(2,6-Dioxopiperidin-3-yl)phthalimidine enhances 1,2-dimethylhydrazine-induction of rat colon adenocarcinomas.

Triptobenzene H (Hypoglic acid) significantly increases TNF-α and IL-1β mRNA levels in macrophages, causing indirect liver damage.

Aloeresin G is a chromone glycoside that can be isolated from Aloe. Aloeresin G has a weak inhibitory effect on TNFα-induced NF-κB transcriptional activity, with an IC 50 value of 40.02 μM.

VR11 aptamer is a DNA-based TNF-α inhibitor with a K_D of 7.0 nM. VR11 aptamer prevents TNFα-induced apoptosis and NO production. VR11 aptamer has non-immunogenicity and does not raise immune responses when injected intraperitoneally into C57BL/6 mice model. VR11 aptamer can be used for inflammatory diseases research.

Hecubine is a monoterpene indole alkaloid found in Ervatamia ocinalis. Hecubine activates TREM2 expression, reduces LPS (HY-D1056)-stimulated inammatory cytokines (TNF-α、IL-6、IL-1β) overexpression, as well as suppresses the levels of TLR4-, MyD88-, MAPK/PI3K/AKT- and NF-κB-related proteins. Hecubin also exhibits antioxidative effect, reduces ROS production and activates of the Nrf2/HO-1 pathway. Hecubine rescues LPS-induced behavioral deficits in zebrash larvae. Hecubine can be used for the research of neural inflammation-associated central nervous system diseases.

Ceftiofur (Standard) is the analytical standard of Ceftiofur (HY-N7102). This product is intended for research and analytical applications. Ceftiofur is a cell wall synthesis inhibitor that targets bacterial penicillin-binding proteins (PBPs) and has anti-inflammatory effects in endotoxemia. Ceftiofur exerts bactericidal effects by inhibiting the synthesis of bacterial cell wall peptidoglycan, leading to bacterial cell lysis. Ceftiofur also inhibits the activation of NF-κB and MAPKs, thereby reducing the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6.

Canventol is an antitumor agent that inhibits the release of TNF-α. Canventol inhibits protein isoprenylation, regulates mevalonate metabolism, enhances Okadaic acid (HY-N6785)-induced early response gene expression, suppresses cell transformation, and inhibits HIV-1 production in infected cells. Canventol can be used in studies related to skin tumor promotion and cancer.

Flurbiprofen axetil (Standard) is the analytical standard of Flurbiprofen axetil. This product is intended for research and analytical applications. Flurbiprofen axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent with anti-inflammatory and analgesic effects. Flurbiprofen axetil inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. Flurbiprofen axetil can promote neuroprotection after focal cerebral ischemia in rats by partially activating PPAR-γ. Flurbiprofen axetil alleviates cerebral ischemia/reperfusion injury by reducing inflammation in a transient global cerebral ischemia/reperfusion rat model. Flurbiprofen axetil can alleviate inflammatory responses and cognitive function in a mild cognitive impairment (MCI) SD rat model through the AMPKα/NF-κB signaling pathway.

Pexmetinib hydrochloride (ARRY-614 hydrochloride) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib hydrochloride 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 hydrochloride 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 hydrochloride can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis.

rel-(1S,2R)-Dihydro bupropion-d₉ hydrochloride is the deuterium labeled rel-(1S,2R)-Dihydro bupropion hydrochloride (HY-178240). rel-(1S,2R)-Dihydro bupropion is a metabolite of bupropion. rel-(1S,2R)-Dihydro bupropion can promote endogenous IL-10 production and inhibit Th1 cytokines (IL-12 and TNF-α). rel-(1S,2R)-Dihydro bupropion can induce immune response transition from Th1 to Th2. rel-(1S,2R)-Dihydro bupropion can be used for research on inflammatory conditions.

Ceftiofur-d₃ sodium is deuterium labeled Ceftiofur sodium (HY-B0898). Ceftiofur sodium is a cell wall synthesis inhibitor that targets bacterial penicillin-binding proteins (PBPs) and has anti-inflammatory effects in endotoxemia. Ceftiofur sodium exerts bactericidal effects by inhibiting the synthesis of bacterial cell wall peptidoglycan, leading to bacterial cell lysis. Ceftiofur sodium also inhibits the activation of NF-κB and MAPKs, thereby reducing the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6.

Mulberroside A (Standard) is the analytical standard of Mulberroside A. This product is intended for research and analytical applications. 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.

TMI-1 (Standard) is the analytical standard of TMI-1 (HY-101448). This product is intended for research and analytical applications. TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions.

Hibiscetin is an orally active anti-inflammatory, antioxidant, antihyperglycemic, hypolipidemic, hepatoprotective and neuroprotective agent. Hibiscetin reduces the levels of TNF-α, IL-1β and IL-6. Hibiscetin inhibits lipid peroxidation, reduces MDA levels, and induces the activities of antioxidant enzymes CAT, GSH and SOD. Hibiscetin lowers blood glucose, reverses reduced insulin levels, regulates adipokine levels, and reduces elevated AST and ALT levels. Hibiscetin alleviates Rotenone (HY-B1756)-induced akinesia and catalepsy, normalizes neurotransmitter levels, and modulates the activities of activated caspase 3 and BDNF. Hibiscetin can be used in the research of type 2 diabetes, Parkinson's disease and Huntington's disease.

5-O-Methylvisammioside (4'-O-β-D-Glucosyl-5-O-methylvisamminol) (Standard) is the analytical standard of 5-O-Methylvisammioside. This product is intended for research and analytical applications. 5-O-Methylvisammioside is an orally active natural chromone glycoside and multiple biological activities. 5-O-Methylvisammioside inhibits ferroptosis by activating the Nrf2/HO-1 signaling axis. 5-O-Methylvisammioside alleviates intestinal barrier damage by inhibiting the ROS/NF-κB/NLRP3 pathway. 5-O-Methylvisammioside exerts a protective effect against acute liver injury by reducing ALT/AST, decreasing inflammatory infiltration, and inhibiting IκB-α phosphorylation and NF-κB nuclear translocation. 5-O-Methylvisammioside blocks the HMGB1/RAGE/MEK/ERK signaling axis to exert anti-tumor and anti-angiogenic effects. 5-O-Methylvisammioside improves depression-like behaviors by inhibiting Src kinase and the NF-κB pathway.

Resatorvid (Standard) is the analytical standard of Resatorvid (HY-11109). This product is intended for research and analytical applications. Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC₅₀s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.

IKK 16 (Standard) is the analytical standard of IKK 16. This product is intended for research and analytical applications. IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC₅₀s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC₅₀s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.

Cornuside (Standard) is the analytical standard of Cornuside (HY-N0631). This product is intended for research and analytical applications. Cornuside is an iridoid glycoside with anti-allergic, anti-inflammatory, and neuroprotective activities. Cornuside exerts anti-allergic activity by downregulating the p38 MAPK, JNK, and NF-κB signaling pathways, and inhibits IgE-mediated histamine release from mast cells. Cornuside improves cognitive impairment in mice by inhibiting BACE1 activity (IC₅₀ = 55.84 μg/mL) and enhancing ChAT activity. Cornuside inhibits LPS (HY-D1056)-induced inflammatory mediators, including iNOS, COX-2, PGE2, TNF-α, IL-6, and IL-1β, by suppressing NF-κB activation.

Paeonidanin is a monoterpenoid glycoside with an IC₅₀ > 100 μM for nitric oxide production inhibition in lipopolysaccharide-activated microglia and macrophages. Paeonidanin suppresses lipopolysaccharide-induced production of nitric oxide, interleukin-6, and tumor necrosis factor alpha in macrophages and microglia.Paeonidanin can be used for the research of inflammation.