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Lipopolysaccharides (LPS) is an endotoxin derived from the outer leaflet of the outer membrane of Gram-negative bacteria. Lipopolysaccharides consists of an antigen O-specific chain, a core oligosaccharide and lipid A. Lipopolysaccharides is a pathogenic associated molecular pattern (PAMP) that activates the immune system. Lipopolysaccharides activates TLR-4 on immune cells . This product is derived from Escherichia coli O55:B5. Lipopolysaccharides induces secretion of cell migrasome .
Vogeloside is an iridoid that can be isolated from the roots of Triosteum pinnatifidum. Vogeloside inhibits nitric oxide production in LPS-activated macrophages .
Bullatantriol ((+)?-?Bullatantriol) can be isolated from the roots of Homalomena aromatica. Bullatantriol can promote the proliferation and differentiation of osteoblasts. Bullatantriol also inhibits LPS-induced NO production in BV2 cells .
RS09 is a LPS peptide mimic serves as a candidate to be considered as a new class of TLR4 agonist adjuvant. RS09 increases antibody production in a vaccine setting .
Moracin C, a natural product, is an anti-inflammatory agent. Moracin C inhibits LPS-activated reactive oxygen species (ROS) and nitric oxide (NO) release from cells .
(+)-14-Deoxy-ε-caesalpin (14-Deoxy-ε-caesalpin), a cassane diterpenoid, inhibits nitric oxide (NO) production release of RAW 264.7 cells stimulated by Lipopolysaccharide (LPS) .
Antimicrobial agent-5 is an potent antimicrobial agent, and displays excellent cell selectivity against Gram-negative bacteria and Gram-positive bacteria. Antimicrobial agent-5 blocks the interaction between LPS and CD14/TLR4 receptor, and shows anti-inflammatory activity against LPS-induced inflammation .
Deoxyandrographolide suppresses LPS induced increase in mRNA levels of iNOS as well as production of proinflammatory mediators TNF-α and IL-6. Deoxyandrographolide potentiates NGF-induced neurite outgrowth .
Berkeleyacetal C, a meroterpenoid compound, shows favorable activity of inhibiting nitrogen oxide (NO) production of macrophages stimulated by lipopolysaccharide (LPS). Berkeleyacetal C exerts anti-inflammatory effects via inhibiting NF-κB, ERK1/2 and IRF3 signaling pathways .
Anti-inflammatory agent 41 (13a) significantly inhibit lipopolysaccharide (LPS)-induced expression of the proinflammatory cytokines IL-6 and TNF-α on J774A.1, THP-1 and LX-2 cells, and inhibits the activation of the NF-κB pathway .
Panobacumab (KBPA101) is a fully human IgM/κ monoclonal antibody generated by immortalizing human B lymphocytes against the LPS O polysaccharide of serotype O11 of P. aeruginosa .
COX-2-IN-32 (Compound 2f) is an iNOS and COX-2 inhibitor. COX-2-IN-32 decreases the expression of NF-κB. COX-2-IN-32 has anti-inflammatory activity by inhibits NO production in LPS-induced RAW264.7 macrophages (IC50: 11.2 μM) .
PDE4-IN-9 (Compound 5j) is a potent inhibitor of PDE4. PDE4-IN-9 exhibits lower IC50 value (1.4 μM) against PDE4 than parent rolipram (2.0 μM) in in vitro enzyme assay. PDE4-IN-9 also displays good in vivo activity in animal models of asthma/COPD and sepsis induced by LPS .
ND-2158 is a competitive IRAK4 inhibitor, with the Ki of 1.3 nM. ND-2158 suppresses LPS-induced TNF production in human white blood cells, alleviated collagen-induced arthritis, and blocked gout formation in mouse models. ND-2158 has antitumor activity in vivo .
iNOS/PGE2-IN-1 (compound 4a), an iNOS/PGE2 inhibitor, is a potent anti-inflammatory agent. iNOS/PGE2-IN-1 can inhibit LPS-induced NO production. iNOS/PGE2-IN-1 possesses low ulcerogenic liabilities .
(4S)-10-Nor-calamenen-10-one (Compound 15) enhances LPS-induced NO production by microglia. (4S)-10-Nor-calamenen-10-one is an eudesmane sesquiterpene that can be isolated from Alpinia oxyphylla .
Telmesteine is an amucolitic agent. Telmesteine has anti-protease activity. Telmesteine inhibits LPS-induced NO production in RAW264.7 cells. Telmesteine can be used for research of inflammation, such as acute and chronic bronchitis and obstructive airways disease .
Loganic acid 6′-O-β-D-glucoside, a iridoidal glucoside, is isolated from the whole plant of Gentiana rhodantha (Gentianaceae). Loganic acid 6′-O-β-D-glucoside inhibits LPS-induced NO and TNF-α production in macrophage RAW264.7 cells .
ONO-3403 is an orally active serine protease inhibitor. ONO-3403 inhibits the production of TNF-α and nitric oxide induced by LPS. ONO-3403 inhibits the cell growth and induces the apoptosis, and has an antitumor effect on malignant tumors .
NF-κB-IN-15 (compound 14r) is a potent NF-κB inhibitor. NF-κB-IN-15 decreases the NO levels and inhibits the release of IL-6, TNF-α, and IL-1β in LPS (HY-D1056) -induced cells. NF-κB-IN-15 inhibits LPS-induced phosphorylation of p65 and degradation of IκBα. NF-κB-IN-15 shows anti-inflammatory activity has the potential for the research of acute lung injury (ALI) .
Hedycoronen A has inhibitory activity on the IL-6, IL-12 p40, and TNF-α production in LPS-Stimulated BMDCs, with IC50s of 9.1 μM, 5.6 μM, and 46.0 μM. Hedycoronen A can be isolated from Hedychium coronarium .
NCI126224 is a TLR4 signaling inhibitor. NCI126224 suppress LPS (HY-D1056)-induced production of NF-κB, TNF-α, IL-1β, and NO in the nanomolar-low micromolar range. NCI126224 can be used for the research of inflammatory diseases .
Articaine (Hoe-045 free base) is an amide anaesthetic containing an ester group, reversibly binding to the α-subunit of the voltage-gated sodium channels within the inner cavity of the nerve, can provide effective pain relief. Articaine ameliorates LPS-induced acute kidney injury via inhibition of NF-ĸB activation and the NLRP3 inflammasome pathway .
Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity .
Zabedosertib (BAY 1834845) is a selective, orally active IRAK4 inhibitor with immunomodulatory potential, IC50 is 3.55 nM. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors . Zabedosertib exhibits anti-inflammatory property against IL-β, LPS (HY-D1056) and Imiquimod (HY-B1080) induced inflammation .
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM .
Articaine hydrochloride (Hoe-045) is an amide anaesthetic containing an ester group, reversibly binding to the α-subunit of the voltage-gated sodium channels within the inner cavity of the nerve, can provide effective pain relief. Articaine hydrochloride ameliorates LPS-induced acute kidney injury via inhibition of NF-ĸB activation and the NLRP3 inflammasome pathway .
NF-κB-IN-8 competitively antagonizes LPS binding to MD-2. NF-κB-IN-8 reduces the expression of inflammatory factors by binding to MD-2. NF-κB-IN-8 also inhibits ALP activity. NF-κB-IN-8 can be used for the research of inflammation such as acute lung injury (ALI) .
Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
BODIPY TR Cadaverine, a cadaverine derivative, is a red fluorescent dye. BODIPY TR Cadaverine can be used in a a highly sensitive and robust fluorescent displacement assay, which binds to native LPS strongly, specifically recognizing lipid A, and is competitively displaced by compounds displaying an affinity for lipid A .
Polymyxin B is an antibiotic. Polymyxin B inhibits Gram-negative infections by binding to the LPS of the bacterial wall with high affinity. Polymyxin B neutralizes the effect of endotoxin. Polymyxin B induces bacterial death by increasing its permeability. Polymyxin B is used in endotoxemia research .
IRAK4-IN-18 is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 value of 15 nM. IRAK4-IN-18 can inhibit LPS-induced IL23 production in THP and DC cells, and stop arthritis development in arthritis rats. IRAK4-IN-18 can be used for researching arthritis disease .
IRAK4-IN-19 is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 value of 4.3 nM. IRAK4-IN-19 can inhibit LPS-induced IL23 production in THP and DC cells, and stop arthritis development in arthritis rats. IRAK4-IN-19 can be used for researching arthritis disease .
(6E)-1,7-Bis(4-hydroxyphenyl)-6-hepten-3-one (compound7) is a nature product isolated from rhizomes of Curcuma kwangsiensis. (6E)-1,7-Bis(4-hydroxyphenyl)-6-hepten-3-one has inhibitory effect on NO production induced by LPS in macrophages with an IC50 value of 8.93 μM .
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation .
BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury .
(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway .
Pep19-2.5 is an synthetic and antitoxin peptide, blocks the intracellular endotoxin signaling cascade. Pep19-2.5 inhibits signaling of lipopeptides (LP) and lipopolysaccharides (LPS) mediated by transmembrane and cytosolic pattern recognition receptors (PRRs). The signaling cascades lead to inflammation and cell pyroptosis .
NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor (IC50= 574 nM) that acts independently of Ca 2+. NLRP3-IN-NBC6 inhibits Nigericin (HY-127019)-induced inflammasome activation in THP-1 cells and Imiquimod (HY-B0180)-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) .
MCTR3 is a potent cytokine of pro-resolving mediating maresin conjugates in tissue regeneration (MCTR), which reduces the inflammatory response and promotes the tissue regeneration. MCTR3 exhibits potency in ameliorating LPS-induced acute lung injury and arthritis .
Catalpalactone has anti-inflammatory effect. Catalpalactone inhibits LPS-induced NO production and iNOS expression in RAW264.7 cells, and also inhibits IRF3, NF-κB, and IFN-β/STAT-1 activation. Catalpalactone also inhibits dopamine biosynthesis by reducing tyrosine hydroxylase (TH) and aromatic-l-amino acid decarboxylase (AADC) activities .
R-HP210 acts on the NF-κB mediated tethered transrepression function (IC50=3.80 μM). R-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. R-HP210 does not induce the transactivation functions of Glucocorticoids (GCs) .
PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor (IC50: 15 nM). PDE1-IN-5 has anti- inflammatory activity, and inhibits expression of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 induced by LPS. PDE1-IN-5 has anti-inflammatory bowel disease (IBD) effects in the dextran sodium sulfate (DSS)-Induced colitis mice model. PDE1-IN-5 can be used for research of IBD .
Delphinidin-3-sambubioside (Dp3‐Sam) chloride is an anthocyanin that has orally active anti-inflammatory activity. Delphinidin-3-sambubioside chloride inhibits LPS-induced inflammatory factors release. Delphinidin-3-sambubioside chloride also alleviates hepatic lipid accumulation in HFD rats. Delphinidin-3-sambubioside chloride can be isolated from Hibiscus sabdariffa L. .
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM .
Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction .
1-Dehydro-[10]-gingerdione directly inhibits IKKβ activity by targeting the activation loop of IKKβ, thus disrupting IKKβ-catalysed IκBα phosphorylation in macrophages stimulated with agonists. 1-Dehydro-[10]-gingerdione inhibits LPS (HY-D1056)-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione has the potential for NF-κB-associated inflammation and autoimmune disorders research .
Protoplumericin A is a bioactive ingredient of Plumeria obtusa L. attenuates. Protoplumericin A mitigated lipopolysaccharide (LPS) -induced acute lung injury in mice. Protoplumericin A can be used to study the LPS-induced anti-inflammatory effect .
JE-133 is an optically active isochromane-2H-chromene conjugate. JE-133 exhibits antioxidant and anti-inflammatory activities. JE-133 is a neuroprotective agent that effectively inhibits neuronal oxidative damage associated with PI3K/Akt and MAPK signaling pathways. JE-133 can also inhibit lipopolysaccharide (LPS) (HY-D1056)-induced neuroinflammation by regulating JAK/STAT and Nrf2 signaling pathways .
Alpinetin is a flavonoid isolated from cardamom and has anti-inflammatory activity. Alpinetin inhibits lipopolysaccharide (LPS)-induced inflammation, activates PPAR-γ, activates Nrf2, and inhibits TLR4 expression to protect LPS-induced renal injury .
GSK-3β inhibitor 15 (Compound 54) is a GSK-3β inhibitor (IC50: 3.4 nM). GSK-3β inhibitor 15 inhibits Aβ1-42-induced GSK-3β and tau protein phosphorylation. GSK-3β inhibitor 15 inhibits LPS-induced iNOS expression. GSK-3β inhibitor 15 has neuroprotective effects on Aβ1-42-induced neurotoxicity. GSK-3β inhibitor 15 can be used for research of Alzheimer’s disease (AD) .
Kdo2-Lipid A ammonium is a chemically defined lipopolysaccharide (LPS) with endotoxin activity equal to LPS. Kdo2-Lipid A ammonium is highly selective for TLR4. Kdo2-Lipid A ammonium stimulates the release of both TNF and PGE2 .
Isogosferol ((+)-Isogospherol; Isogospherol) is a potent anti-inflammatory agent. Isogosferol decreases LPS (HY-D1056)-stimulated NO and IL-1β expression. Isogosferol decreases the LPS (HY-D1056)-stimulated expression of iNOS, COX-2, NF-κB, and pERK1/2 .
Taxamairin B is a potent anti-inflammatory agent. Taxamairin B decreases proinflammatory cytokines (TNF-α, IL-1β and IL-6) expression and the production of NO and ROS in LPS-induced RAW264.7 cells. Taxamairin B exhibits significant
protective effects in LPS-induced acute lung injury in mice .
20-Hydroxyganoderic Acid G is a lanostane triterpenoid obtained from the EtOH extract of fruiting bodies of the Ganoderma curtisii. 20-Hydroxyganoderic Acid G inhibits BV-2 microglia cells activated by LPS with an IC50 of 21.33 μM. 20-Hydroxyganoderic Acid G has therapeutic potential in the agent discovery of nerve inflammation diseases associated with microglia activated by LPS .
Chitohexaose hexahydrochloride is a chitosan oligosaccharide with anti-inflammatory effect. Chitohexaose hexahydrochloride binds to the active sites of TLR4 and inhibits LPS induced inflammation .
Randaiol is an antioxidant that can be isolated from the stem bark of Magnolia officinalis. Randaiol inhibits LPS-induced NO production and has anti-inflammatory and antioxidant activities .
Diplacol ia a natural compound from from Mimulus clevelandi and shows potent inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide production .
RO7075573 (compound 3) is an antibiotics that targets the lipopolysaccharide (LPS) transport machine in Acinetobacter. RO7075573 protects mice from A. baumannii infections .
Isomaculosidine is an alkaloid that can be isolated from D. dasycarpus. Isomaculosidine can inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated BV2 microglial cells .
Anti-inflammatory agent 7 inhibits proinflammatory cytokines by blocking the NF-κB/MAPK signaling pathway in LPS-treated RAW 264.7 cells as well as mice.
O-Acetylschisantherin L (Acetylschisantherin L) is a natural lignan, which exhibits inhibitory effects on LPS-induced NO production in BV-2 cells with an IC50 of 23.1 μM .
Anhydronotoptol is a potent nitric oxide inhibitory coumarin. Anhydronotoptol inhibits NO production in RAW 264.7 cells induced by LPS with an IC50 value of 36.6 μM .
Lonicerin is an anti-algE (alginate secretion protein) flavonoid with inhibitory activity for P. aeruginosa. Lonicerin prevents inflammation and apoptosis in LPS-induced acute lung injury .
Maresin 1, produced by human Mφs from endogenous docosahexaenoic acid (DHA) and a specialized proresolving mediator, stimulates intracellular [Ca 2+] and secretion. Maresin 1 possesses anti-inflammatory activity .
(3β,24S)-3-Hydroxystigmast-5-en-7-one (Compound 31) is a compound that can be isolated from Lindera akoensis . (3β,24S)-3-Hydroxystigmast-5-en-7-one has anti-inflammatory activity .
Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways .
Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity .
Herpotrichone A shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.41 μM.
Curindolizine, indolizine alkaloid , displays an anti-inflammatory action in lipopolyssacharide (LPS)-induced RAW 264.7 macrophages with an IC50 value of 5.31 μM .
Hyuganin D (Isobocconin) is a Coumarin (HY-N0709) constituent that substantially inhibits LPS (HY-D1056)-induced NO production in mouse peritoneal macrophages .
Neocurdione is a hepatoprotective sesquiterpene isolated from Curcuma zedoaria rhizome. Neocurdione exerts potent effect on D-galactosamine- (D-Gain) and lipopolysaccharide- (LPS) induced acute liver injury in mice .
3-O-Acetyl-16α-hydroxydehydrotrametenolic acid, an anti-inflammatory triterpenoid, inhibits NO production and iNOS expression in LPS-stimulated Raw264.7 cells .
Herpotrichone B shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.11 μM.
Chloranthalactone E (compound 6), a labdane diterpene, can be isolated from the aerial parts of Chloranthus serratus. Chloranthalactone E inhibits NO production in LPS-activated RAW 264.7 macrophages .
Vitexdoin A is a nitric oxide scavenging lignin. Vitexdoin A inhibits NO production with an IC50 of 0.38 μM in LPS (HY-D1056)-stimulated RAW 264.7 cells .
C5 Lenalidomide (Lenalidomide 5'-amine) is a thalidomide analog and is a potent inhibitor of TNF-alpha production (IC50=100 μM in LPS stimulated human PBMC) .
12-Dehydrogingerdione is an inhibitor of NO Synthase. 12-Dehydrogingerdione signi?cantly inhibits LPS-stimulated production of NO, IL-6 and PGE2 in Raw 264.7 cells .
Isomucronulatol is a flavonoid isolated from the roots of A. membranaceus. Isomucronulatol exhibits inhibitory effects on LPS-stimulated production IL-12 p40 in vitro and has potential anti-inflammatory effect .
Inflexuside B, an abietane diterpenoid, can be isolated from the aerial parts of Isodon inflexus. Inflexuside B strongly inhibits lipopolysaccharide (LPS)-activated NO Synthase in RAW264.7 macrophages .
Inflexuside A, an abietane diterpenoid, can be isolated from the aerial parts of Isodon inflexus. Inflexuside B strongly inhibits lipopolysaccharide (LPS)-activated NO production (NO Synthase) in RAW264.7 macrophages .
Phaeocaulisin E (Compound 5) is a guaiane-type sesquiterpene that inhibits LPS HY-(HY-D1056)-induced NO production in RAW 264.7 macrophages with an IC50 of 10.3 μM .
Kanshone B (Compound 5) is isolated from the
natural Nardostachys chinensis. Kanshone B shows inhibitory
activity against LPS-induced NO production (IC50=11.5 μM)
.
Andropanolide is a natural product that exerts cytotoxicity toward carcinoma cells and significantly inhibits the overproduction of nitric oxide (NO) in Lipopolysaccharides (HY-D1056) (LPS)-stimulated RAW264.7 macrophages .
Epimagnolin B is a bisepoxylignan isolated from Magnolia fargesii, with anti-inflammatory activity and antiallergic effects. Epimagnolin B inhibits NO production in LPS-activated microglia. Epimagnolin B exhibited antiallergic effects .
Licoagrochalcone C, a flavonoid, reveals efficacious inhibitory activity on NF-κB transcription. Licoagrochalcone C shows significant inhibitory activity on LPS (HY-D1056)-induced NO production .
9-Hydroxy-α-lapachone (α-Dihydrocaryopterone) is a natural phenol, exhibits potent inhibitory effects with an IC50 of 4.64 µM on LPS-induced NO production in RAW 264.7 cells .
N-cis-Feruloyl tyramine (cis-N-(4-Hydroxyphenethyl) ferulamide) is a natural phenolic compound, exhibits modest inhibitory activity on LPS-activated NO production in RAW 264.7 cells .
DBM 1285 dihydrochloride is an orally active TNF-α production inhibitor with anti-inflammatory effects. DBM 1285 dihydrochloride inhibits Lipopolysaccharide (LPS)-induced TNF-α secretion in various cells of macrophage/monocyte lineage .
Inubritannolide A displays slight strong neuroprotective potency against different types of neuronal cells mediated by various inducers including H2O2, 6-hydroxydopamine (6-OHDA), and lipopolysaccharide (LPS).
Guaiacol-d3 is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Guaiacol has an anti-inflammatory activity[1].
Sibiricine (Compound 8) is an isoquinoline alkaloid derived from the medicinal plant Corydalis crispa. Sibiricine has significant anti-inflammatory activity on TNF-α production by LPS-activated THP-1 cells .
NF-κB/MAPK-IN-1 (compound 11a) is a potent inhibitor of NF-κB and MAPK pathway. NF-κB/MAPK-IN-1 shows inhibitory activity against NO production, with an IC50 of 6.96 µM. NF-κB/MAPK-IN-1 suppresses LPS-induced iNOS, COX-2, ERΚ and P38 signaling activation. NF-κB/MAPK-IN-1 can prevent LPS induced inflammatory response in macrophages. NF-κB/MAPK-IN-1 can be used for rheumatoid arthritis (RA) research .
Plantamajoside is a phenylpropanoid glycoside isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside has protective effects on LPS-induced acute lung injury (ALI) mice model. Plantamajoside has the potential for the treatment of pulmonary inflammation .
Dehydroandrographolide can be extracted from herbal medicine Andrographis paniculata Nees. Dehydroandrographolide reduces oxidative stress in LPS-induced acute lung injury by inactivating iNOS. Dehydroandrographolide has anti-infective activity .
TBT1 is a first-generation inhibitor of the MsbA transporter. TBT1 is an LPS transport inhibitor and MsbA ATPase stimulator in strains from the Acinetobacter genus. TBT1 stimulated ATPase activity with an EC50 of 13 µM .
Sugiol is an abietane diterpenoid, can be isolated from Calocedrus formosana bark. Sugiol has anti-inflammatory activity, could effectively reduce intracellular reactive oxygen species (ROS) production in lipopolysaccharide (LPS)-stimulated macrophages .
Hyperelamine A (compound 5) is a polycyclic polyprenylated acylphloroglucinols (PPAPs). Hyperelamine A exhibits inhibitory activity against LPS-activated NO production in BV-2 cells via TLR-4/NF κB signaling .
Guaiacol (Standard) is the analytical standard of Guaiacol. This product is intended for research and analytical applications. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation . Anti-inflammatory activity .
Bermoprofen (AD-1590) is an orally active non-steroidal anti-inflammatory agent. Bermoprofen has potent antipyretic activities with a short biological half-life. Bermoprofen is a potent antagonist of LPS-induced fever in rabbits .
15a-Hydroxy-3,11,23-trioxo-lanost-8,20-dien-26-oic acid, a Lanostane triterpenoid, possesses NO production inhibitory activities of LPS-induced microglia .
EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation .
Geranylgeraniol is an orally acitve vitamin K2 sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model .
Guaiacol-d7 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Guaiacol-d4 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Motapizone (NAT 05-239) is a selective PDE3 inhibitor. Motapizone moderately inhibits cytokine release in lipopolysaccharide (LPS)-induced alveolar macrophages. Motapizone also inhibits human platelet aggregation by increasing intracellular cAMP .
NF-κB-IN-13 (compound 12) can significantly inhibit LPS-induced NF-κB activation and NO production in RAW264.7 macrophages. NF-κB-IN-13 has anti-inflammatory effects .
Saucerneol is a lignans that can be isolated from Saururus chinensis. Saucerneol inhibits LPS-induced or Con A-induced lymphocytes proliferation. Saucerneol inhibits mixed lymphocyte response. Saucerneol also inhibits mitogens-induced cytokines secretion .
KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH .
Etiprednol dicloacetate (BNP 166) is an anti-inflammatory agent. Etiprednol dicloacetate inhibits eosinophil accumulation. Etiprednol dicloacetate can be used in the research of inflammatory airway diseases, such as asthma .
Isodorsmanin A is an anti-inflammatory agent. Isodorsmanin A suppresses the production of inflammatory mediators and proinflammatory cytokines. Isodorsmanin A inhibits the phosphorylation of JNK, MAPK .
Esculentic acid is a selective COX-2 inhibitor and has anti-inflammatory effect. Esculentic acid is a pentacyclic triterpenoid that can be extracted from the Chinese herb Phytolacca esculenta .
Docosahexaenoyl serotonin (DHA-5-HT) is an endogenous n-3 fatty acid-serotonin conjugate. Docosahexaenoyl serotonin is an inhibitor of IL-17. Docosahexaenoyl serotonin has anti-inflammatory activity .
BET-IN-8 (Compound 27) is a potent inhibitor of BET with a Ki and Kd of 0.83 and 0.571 μM, respectively. BET-IN-8 ameliorates LPS-induced sepsis in vivo. BET-IN-8 has the potential for the research of sepsis .
Damnacanthol is a natural product that can be isolated from Damnacanthus major . Damnacanthol has anti-15-lipoxygenase activity and can inhibit nitric oxide production in LPS-activated macrophages RAW 264.7 cells .
Guaiacol- 13C6 is the 13C labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Guaiacol-d4-1 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Anti-inflammatory agent 63 is an anti-inflammatory agent that shows optimal inhibitory activity (EC50 = 5.33±0.57 μM) against the production of nitric oxide (NO) induced by lipopolysaccharide (LPS) in RAW264.7 cells .
(Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation .
8-Methylsulfinyloctyl isothiocyanate, an isothiocyanate, has antimicrobial activity and remarkable inhibitory activity against plant growth . 8-Methylsulfinyloctyl isothiocyanate impair COX-2 mediated inflammatory responses in LPS stimulated raw macrophages .
Org 48762-0 is a potent, orally active and selective p38 inhibitor with EC50 of 0.1 μM. Org 48762-0 reduces LPS-induced TNFα release and prevents bone damage in collagen-induced arthritis in mice .
KC01 is an effective inhibitor of ABHD16A, with IC50s of 90 nM for hABHD16A and 520 nM for mABHD16A. KC01 significantly reduces lyso-PSs, and decreases lyso-PS and LPS-induced cytokine production in mouse macrophages .
Chebulanin, a polyphenol acid, exerts its anti-inflammatory and anti-arthritic effects via inhibiting NF-κB and MAPK activation in collagen-induced arthritis mice. Chebulanin inhibits the nuclear translocation of p38 and p65 in LPS-stimulated macrophages .
Inulicin (1-O-Acetylbritannilactone) is an active compound that inhibits VEGF-mediated activation of Src and FAK. Inulicin (1-O-Acetylbritannilactone) inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
Bisabolangelone, a sesquiterpene derivative, is isolated from the roots of Osterici Radix. Bisabolangelone possesses anti-inflammatory properties, which inhibits LPS-stimulated inflammation through the blocking of NF-kappaB and MAPK pathways in macrophages. Bisabolangelone has anti-ulcer activities .
Anti-inflammatory agent 42 (Compound 10j) is an anti-inflammatory agent. Anti-inflammatory agent 42 shows excellent inhibition on the expression of TNF-α and IL-6 in LPS (HY-D1056)-stimulated macrophages .
α-Glucosidase-IN-37 (Compound 11) moderately inhibits LPS-induced NO production with an IC50 value of 23.7 μM in macrophages. α-Glucosidase-IN-37 has weak inhibitory activity against α-Glucosidase .
Diplacol is a geranylated flavanone that can be isolated from paulownia trees (Paulownia coreana UYEKI). Diplacol has anti-inflammatory activity. Diplacol inhibits NO production in LPS-stimulated Raw264.7 cells with an IC50 value of 4.53 μM .
Erdosteine- 13C4 is a 13C-labeled Erdosteine. Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation[1][2]. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects[3].
Beclometasone dipropionate-d10 is the deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
Beclometasone dipropionate-d6 is deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
Anti-inflammatory agent 23 (Compound 4m) is an anti-inflammatory agent. Anti-inflammatory agent 23 inhibits the production of NO activated by LPS with an IC50 of 0.449 μM. Anti-inflammatory agent 23 has a good affinity for p65 protein .
Asperbisabolane L, a sesquiterpenoid, exerts the anti-inflammatory activity by inhibiting the NF-κB-activated pathway. Asperbisabolane L inhibits the translocation of NF-κB from cytoplasm to the nucleus. Asperbisabolane L also inhibits NO production in LPS-activated BV-2 microglia cells .
STING-IN-5 is a potent STING inhibitor, inhibiting LPS-induced NO synthesis in macrophages with an IC50 value of 1.15 μM. STING-IN-5 inhibits the inflammatory response. STING-IN-5 can be used to research anti-inflammatory diseases and sepsis .
Pratol is a potent inhibitor of NF-κB. Pratol significantly reduces NO and prostaglandin PGE2 production without any cytotoxic in LPS-stimulated RAW 264.7 cells. Pratol reduces proinflammatory cytokines. Pratol can be used in study inflammatory diseases and cancer .
Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 inhibits VCAM-1 and ICAM-1 expressions stimulated with lipopolysaccharide (LPS). Ginsenoside Rg2 also reduces Aβ1-42 accumulation.
Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
Isomucronulatol 7-O-glucoside is a flavonoid isolated from the roots of A. membranaceus. Isomucronulatol 7-O-glucoside exhibits weak inhibitory effects on LPS-stimulated production IL-12 p40 in vitro and has potential anti-inflammatory effect .
PHA 408 (PHA-408) is a potent, selective and orally active IκB kinase-2 (IKK-2) inhibitor. PHA 408 is a powerful anti-inflammatory agent against lipopolysaccharide (LPS)- and cigarette smoke (CS)-mediated lung inflammation .
Shegansu B is an inhibitor of IL-1β. Shegansu B 6 inhibits IL-1β expression on LPS-induced THP-1 cells with 64.74% inhibition. Shegansu B has anti-inflammatory activity .
A3373, a novel chemical inhibitor of Phospholipase D1 (PLD1) and PLD2, with IC50 of 325 nM and 15.15?μM, respectively, inhibits LPS-induced immune response and plays important roles in autoimmune arthritis, bone demineralization and osteoclastogenesis .
13-Methylberberine chloride (13-Methylberberinium chloride), a berberine analogue, has anti-adipogenic and antitumor activities. 13-Methylberberine chloride (13-Methylberberinium chloride) increases production of IL-12 and inhibits the expression of iNOS at posttranscriptional level in macrophages activated with LPS .
JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages .
Methyl everninate is the major constituent of the deuterochloroform. Methyl everninate, rhodomollosides A and B are the derivatives of Methyl everninate, with cytotoxicity against RAW264.7 cells. Both of they shows inhibitory effects with a lipopolysaccharide (LPS)-stimulated murine macrophages RAW 264.7 cells model .
Anti-inflammatory agent 66 (compound 8) is a pterostilbene derivative with anti-inflammatory activity. Anti-inflammatory agent 66 inhibits pro-inflammatory cytokines by blocking the LPS-induced NF-κB/MAPK signaling pathway and effectively alleviates DSS-induced acute colitis in mice .
Sunset Yellow FCF (Orange Yellow S) is an orange azo dye with a maximum absorption wavelength of 480 nm. Sunset Yellow FCF can be used in food, cosmetics and pharmaceuticals .
Absinthin is a structurally unique triterpene, and is responsible for the high bitter value of wormwood. Absinthin is an agonist of the bitter taste receptor hTAS2R46, which reduces cytosolic Ca 2+-rises induced by histamine by a receptor-specific mechanism mediated by hTAS2R46 .
p38 MAP Kinase Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC50s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively .
Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40 .
PI3Kδ-IN-14 (Compound (S)-29) is a selective PI3Kδ inhibitor (IC50: 0.8 nM, Kd: 84.8 nM). PI3Kδ-IN-14 binds to the ATP-binding site of the kinase domain of PI3Kδ. PI3Kδ-IN-14 has anti-inflammatory activity by inhibiting the PI3K/AKT pathway. PI3Kδ-IN-14 ameliorates acute lung injury (ALI) .
25S-Inokosterone is a phytoecdysone in the roots of two same species of A. bidentata Blume and A. japonica Nakai, and two different species of C. capitata Moq and C. officinalis Kuan. 25S-Inokosterone has the potential for the LPS-induced acute kidney injury research .
iNOs-IN-1 (YPW) is a potent inducible nitric oxide synthase (iNOS) inhibitor. iNOs-IN-1 can significantly inhibit the expression of IL-6 and iNOS, as well as reduce LPS-induced NO generation with dose-dependent manner in mouse macrophages. Anti-inflammatory effects .
Anti-inflammatory agent 12 (Compound 2) is a pentacyclic triterpene compound. Anti-inflammatory agent 12 shows a significant bias in the LPS-induced inflammatory response with an IIC50 value of 2.22 μM. Anti-inflammatory agent 12 has the potential for the research of inflammation disease .
iNOs-IN-3 (Compound 2d) is an orally active nitric oxide synthase (iNOS) inhibitor (IC50=3.342 µM). iNOs-IN-3 shows anti-inflammatory activity and can be used in LPS-induced acute lung injury (ALI) research .
Apiin, a major constituent of Apium graveolens leaves with anti-inflammatory properties. Apiin shows significant inhibitory activity on nitrite (NO) production (IC50 = 0.08 mg/mL) in-vitro and iNOS expression (IC50 = 0.049 mg/ mL) in LPS-activated J774.A1 cells .
Kauran-16,17-diol (ent-Kauran-16β,17-diol), a natural diterpene, posseses anti-tumor and inducing-apoptosis activity, with a IC50 of 17 μM on inhibiting NO production in LPS-stimulated RAW 264.7 macrophages .
GSK761 is a selective inhibitor of speckled 140 kDa (SP140) with an IC50 value of 77.79 nM. GSK761 reduces monocyte-to-inflammatory macrophage differentiation and lipopolysaccharide (LPS)-induced inflammatory activation. GSK761 induces the production of CD206 + regulatory macrophages by inhibiting SP140 .
M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis .
CGA-JK3 is CGA-JK3 is an ATP-competitive inhibitor of IKKβ-catalyzed kinase activity. CGA-JK3 inhibits IκBα phosphorylation in LPS (HY-D1056) - induced RAW 264.7 cells .
L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a high affinity and low KD value of 33.3 μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC50 values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research .
Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
12-Oxo phytodienoic acid (12-OPDA) is a plant lipid-derived anti-inflammatory compound. 12-Oxo phytodienoic acid suppresses neuroinflammation by inhibiting Nf-κB and p38 MAPK signaling in LPS-activated cells. 12-Oxo phytodienoic acid can be used for neurodegenerative diseases research .
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation .
Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes . Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells .
Luteolin 5-O-glucoside, a major flavonoidfrom Cirsium maackii, possesses anti-inflammatory activity. Luteolin 5-O-glucoside inhibits LPS-induced NO production and t-BHP-induced ROS generation. Luteolin 5-O-glucoside suppresses the expression of iNOS and COX-2 in macrophages .
Isoforskolin is the principle active component of C. forskohlii native to China. Isoforskolin reduces the secretion of lipopolysaccharide (LPS)-induced cytokines, namely TNF-α, IL-1β, IL-6 and IL-8, in human mononuclear leukocytes. Isoforskolin acts as an anti-inflammatory agent for the treatment of Lyme arthritis .
BMS-751324 is a p38α MAPK inhibitor. BMS-751324 equips a precursor of carbamyl-methyl linkage, containing esters and phosphate functional groups derived from hydroxyphenylacetic acid (HPA). BMS-751324 effectively inhibits foot swelling and LPS-induced TNFα production in an arthritic rat model .
Sanggenon A (Sanggenone A) exerts anti-inflammatory effects by regulating NF-κB and HO-1/Nrf2 signaling pathways in BV2 and RAW264.7 cells. Sanggenon A markedly inhibits the Lipopolysaccharide (LPS; HY-D1056)-induced production of nitric oxide .
Nyasol ((-)-Nyasol) is an active compound that has antifungal, antibacterial, antileishmanial, hyaluronidase inhibition activities. Nyasol inhibits LTB4 binding to human neutrophils. Nyasol suppresses neuroinflammatory response through the inhibition of I-κB degradation in LPS (HY-D1056)-stimulated BV-2 microglial cells .
SpHistin is an antimicrobial peptide (AMP). SpHistin can bind to LPS (HY-D1056) and permeabilize the bacterial membrane. SpHistin combined with Rifampicin (HY-B0272) and Azithromycin (HY-17506) promotes the intracellular uptake of the antibiotics and subsequently enhances the bactericidal activity of both agents against P. aeruginosa .
7-Deacetylgedunin is an activator of Keap1/Nrf2/HO-1. 7-Deacetylgedunin alleviates mice mortality induced by LPS. 7-Deacetylgedunin inhibits Keap1 expression and suppresses macrophage proliferation. 7-Deacetylgedunin suppresses inflammation in vivo and in vitro .
Cavidine ((+)-Cavidine) is a selective COX-2 inhibitor which possesses anti-inflammatory activity. Cavidine can be used for the research of skin injuries, hepatitis, cholecystitis, and scabies. Cavidine ameliorates LPS (HY-D1056)-induced acute lung injury via NF-κB signaling pathway .
Ruscogenin suppresses HCC metastasis by reducing the expression of MMP-2, MMP-9, uPA, VEGF and HIF-1α via regulating the PI3K/Akt/mTOR signaling pathway . And Ruscogenin alleviates LPS-induced pulmonary endothelial cell apoptosis by su
Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain .
SRTCX1002 is a potent activator of SIRT1 (STAC), suppresses inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB Activity. SRTCX1002 suppresses stimuli-induced NF-κB transcriptional activation and LPS-induced TNFα secretion with IC50s of 0.71 and 7.58 µM, respectively .
NF-κB-IN-6 (Compound 3d) is an anti-inflammatory agent through the mechanism of decreasing the protein expressions of iNOS and COX-2 by suppressing NF-κB signaling pathway. NF-κB-IN-6 inhibits NO production in LPS-induced RAW264.7 cells with an IC50 of 23.1 μM .
Nrf2 activator-5 (compound 1) is a potent Nrf2 activator that can attenuate H2O2-induced oxidative stress and LPS-stimulated inflammation in BV-2 microglial cells. Nrf2 activator-5 exhibits antioxidant and anti-inflammatory activities .
CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM. CAY10614 can improve survival of mice in lethal endotoxin shock model .
Anti-inflammatory agent 38 (compound 23d) is a potent Nrf2/HO-1 pathway inhibitor, with an IC50 value of 0.38 μM for NO. Anti-inflammatory agent 38 can significantly reduce the level of ROS in cells. Anti-inflammatory agent 38 can be used for researching anti-inflammatory .
Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases .
Nerandomilast (BI 1015550) dihydrate is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD) .
Nerandomilast (BI 1015550) is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD) .
Oxalomalic acid (Oxalomalate) trisodium is a aconitase and NADP-dependent isocitrate dehydrogenase inhibitor. Oxalomalic acid trisodium inhibits nitrite production and iNOS protein expression in lipopolysaccharide (HY-D1056)-activated J774 macrophages .
SKF-86002 is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid .
Cimifugin (Cimitin) is a bioactive component of Cimicifuga racemosa, a Chinese herb. Cimifugin suppresses allergic inflammation by reducing epithelial derived initiative key factors via regulating tight junctions . Cimifugin reduces the migration and chemotaxis of RAW264.7 cells and inhibits the release of inflammatory factors and activation of MAPKs and NF-κB signaling pathways induced by LPS .
6-Hydroxyflavone is a naturally occurring flavone, with anti-inflammatory activity. 6-Hydroxyflavone exhibits inhibitory effect towards bovine hemoglobin (BHb) glycation. 6-Hydroxyflavone can activate AKT, ERK 1/2, and JNK signaling pathways to effectively promote osteoblastic differentiation. 6-Hydroxyflavone inhibits the LPS-induced NO production .
α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects .
SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid .
Anti-inflammatory agent 20 (compound 5a) is a potent inhibitor of NO activity. Anti-inflammatory agent 20 shows anti-inflammatory activity. Anti-inflammatory agent 20 suppresses LPS-induced inflammation via inhibiting the activation of NF-κB and MAPK signaling and thereby reducing IL-6, TNF-α, iNOS, and COX-2 upregulation .
Vitisin A has antioxidative, anticancer, antiapoptotic, neuroprotective and anti-inflammatory effects. Vitisin A inhibits LPS-induced NO and iNOS production via down-regulation of ERK1/2 and p38 and the NF-κB signal pathway. Vitisin A also inhibits adipocyte differentiation. Vitisin A is a resveratrol tetramer that can be isolated from Vitis vinifera roots .
Sarglaroids F (compound 6) is an anti-inflammatory agent isolated from the roots of Grass Coral. Sarglaroids F inhibits LPS/ATP-induced IL-1β release by affecting K+ efflux and reducing Caspase-1(P20) levels. Sarglaroids F is not cytotoxic to RAW264.7 cells .
Bis-5,5-Nortrachelogenin is isolated from active extract of root of Wikstroemia indica. Bis-5,5-Nortrachelogenin inhibits nitric oxide (NO) production in a lipopolysaccharide (LPS) and recombinant mouse interferon-γ(IFN-γ) activated murine macrophage-like cell line, RAW 264.7 with an IC50 value of 48.6 mM .
Isozaluzanin C (Dehydrozaluzanin c-derivative) is an anti-inflammatory agent that can be isolated from Saussurea lappa and has immunomodulatory effects. Isozaluzanin C improves tissue damage (lung, kidney, and liver) and excessive inflammation in mice induced by LPS (HY-D1056) or CRKP infection. Isozaluzanin C can be used in the study of bacterial infections and sepsi .
AMPK-IN-5 (compound 7m) is a Osthole (HY-N0054) derivative, and blocks MAPK signal transduction by inhibiting the phosphorylation of JNK and p38, thereby inhibiting the release of inflammatory cytokines. AMPK-IN-5 reduce DSS-induced ulcerative colitis and LPS (HY-D1056)-induced acute lung injury .
Tolfenamic acid- 13C6 is the 13C6 labeled Tolfenamic acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
Shizukaol B is a lindenane-type dimeric sesquiterpene, used to be isolated from the whole plant of Chloranthus henryi. Shizukaol B has anti-inflammatory effect against lipopolysaccharide (LPS)-induced activation of BV2 microglial cells. Shizukaol B inhibits iNOS and COX-2, and suppresses NO production, TNF-α, and IL-1β expression .
Broussochalcone A is an antioxidant and an inhibitor of Xanthine Oxidase (IC50=2.21 μM), with free radical scavenging activity. Broussochalcone A inhibits iron-induced lipid peroxidation and nitric oxide synthesis in lipopolysaccharide (LPS) -activated macrophages. Broussochalcone A also induces Apoptosis of human renal carcinoma cells by increasing ROS levels and activating FOXO3 signaling pathways .
CIAC001 is a Pyruvate Kinase PKM2 inhibitor with anti-neuroinflammatory activity. CIAC001 inhibits LPS-induced proinflammatory nitric oxide (NO) production and protects immunologically active BV-2 cells (IC50=2.5 μM). CIAC001 also has anti-neuroinflammation in mouse models and inhibits chronic morphine-induced addiction .
Fortunellin, is a flavonoid, that can be isolated from the fruits of Fortunella margarita (kumquat). Fortunellin exhibits little toxicity to mice and suppresses inflammation and ROS generation in H9C2 cells induced by LPS. Fortunellin protects against fructose-induced inflammation and oxidative stress by enhancing AMPK/Nrf2 pathway. Fortunellin can be used for diabetic cardiomyopathy research .
Thonzonium bromide is an antibacterial agent that is structurally similar to Farnesol (HY-Y0248A). Thonzonium bromide is also a monocationic surface-active agent, which inhibits RANKL-induced osteoclast formation and bone resorption in vitro and prevents LPS-induced bone loss in vivo. Thonzonium bromide inhibits proton transport in a dose-dependent manner (EC50=69 μM) .
Acetylspiramycin (Spiramycin B) is an effective oral macrolide antibiotic produced by Streptomyces, It can inhibit the splenic lymphocyte transformation induced by phytohemagglutinin (PHA), LPS (HY-D1056) and antigen, reduce the procoagulant activity of macrophages, have good antibacterial effect on gram-positive bacteria, and is also an effective antigenic insect agent, which can be used to fight parasitic infection .
Tolfenamic acid-d4 is the deuterium labeled Tolfenamic Acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1[1][2].
L48H37 is an analog of Curcumin (HY-N0005) with improved chemical stability. L48H37 is a potent and specific myeloid differentiation protein 2 (MD2) inhibitor and inhibits the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is used for the research of sepsis or lung injury treatment .
Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells .
Dihydrolipoic Acid (DHLA) is an excellent antioxidant capable of scavenging almost any oxygen-centered radical . Dihydrolipoic acid exhibits anti-inflammatory properties in various diseases. Dihydrolipoic Acid exerts a preventive effect via ERK/Nrf2/HO-1/ROS/NLRP3 pathway in LPS-induced sickness behavior rats. Dihydrolipoic Acid can be used for the reaserch of depression .
TMI-1 is a potent inhibitor of disintegrin metalloenzyme 17 (ADAM17) and other MMPs. TMI-1 inhibits LPS-induced TNF-α secretion in human primary monocytes, and human whole blood . TMI-1 selectively induces caspase-dependent apoptosis in triple negative (TN) and ERBB2-overexpressing breast tumor cell lines .
Anti-inflammatory agent 22 (compound 14a) is an orally active anti-inflammatory agent. Anti-inflammatory agent 22 inhibits LPS-induced TNF-α production with an IC50 value of 14.6 μM. Anti-inflammatory agent 22 has preventive effects on lymphedematous tissue via suppression of adipogenesis. Anti-inflammatory agent 22 suppresses limb lymphedema volume in mice .
Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein .
Ginsenoside Rg2 (Standard) is the analytical standard of Ginsenoside Rg2. This product is intended for research and analytical applications. Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 inhibits VCAM-1 and ICAM-1 expressions stimulated with lipopolysaccharide (LPS). Ginsenoside Rg2 also reduces Aβ1-42 accumulation.
Tolfenamic Acid (Standard) is the analytical standard of Tolfenamic Acid. This product is intended for research and analytical applications. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor .
Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects .
NF546 is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 stimulates release of interleukin-8 from human monocyte-derived dendritic cells .
HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2 .
2-Aminofluorene is a synthetic chemical insecticide. 2-Aminofluorene is a genotoxin. 2-Aminofluorene can be used in the research of DNA adduct structure, DNA repair, carcinogenesis, and mutagenesis .
Tiprelestat is a potent human neutrophil elastase inhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease .
Hispolon, a polyphenol, can be isolated from Phellinus linteus. Hispolon possesses anticancer, antidiabetic, antioxidant, antiviral, hepatoprotective, anti-diabetic, and anti-inflammatory activities .
NF546 (hydrate) is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 (hydrate) stimulates release of interleukin-8 from human monocyte-derived dendritic cells .
COX-2/15-LOX-IN-5 (Compound 4f) is a dual inhibitor of COX-2/15-LOX. COX-2/15-LOX-IN-5 attenuates increased NF-κB activation in RAW 264.7 macrophages mediated by lipopolysaccharide (HY-D1056). COX-2/15-LOX-IN-5 has anti-inflammatory and antioxidant activities .
Coniferaldehyde (4-Hydroxy-3-methoxycinnamaldehyde) is an effective inducer of heme oxygenase-1 (HO-1). Coniferaldehyde inhibits LPS-induced apoptosis through the PKCα/β II/Nrf-2/HO-1 dependent pathway in RAW264.7 macrophage cells. Coniferaldehyde has antioxidant and anti-inflammatory activities .
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure .
JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice . JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM .
Britannilactone diacetate (1,6-O,O-Diacetylbritannilactone; Compound 2) exhibits potential NO inhibition effect. Britannilactone diacetate exhibits activity against NO production induced by LPS in BV-2 microglial cells with the EC50 value of 6.3 μM. Britannilactone diacetate exhibits a favorable blood-brain barriers (BBB) penetration and absorption, distribution, metabolism, excretion, and toxicity (ADMET) property .
Nrf2 activator-8 (compound 10e) is a Nrf2 activator (EC50=37.9 nM). Nrf2 activator-8 exhibits remarkable antioxidant and anti-inflammatory effects in BV-2 microglial cells. Nrf2 activator-8 can significantly restore spatial memory deficits in a mouse model of lipopolysaccharide (LPS)-induced neuroinflammation .
Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibits the IKK Complex. Wedelolactone also inhibits 5-lipoxygenase (5-Lox) with an IC50 of 2.5 μM. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Wedelolactone can extract from Eclipta alba, and it can be used for the research of cancer .
Lewis X trisaccharide (Lewis X, Le x) is a potent TH2 regulator, antagonizes LPS-induced IL-12 immune expression. Lewis X trisaccharide is a human histo-blood group antigen, plays an key role in cell-cell adhesion, and servers as a tumor marker. Lewis X trisaccharide is highly expressed in the outer membrane of the parasite, can be used for the immunology research of schistosomiasis .
SIRT5 inhibitor 7 (compound 58) is a substrate-competitive and selective SIRT5 inhibitor with anti-inflammatory activity. SIRT5 inhibitor 7 has renal protective effects and regulates protein succinylation and the release of pro-inflammatory cytokines. SIRT5 inhibitor 7 has in vivo activity in AKI mouse models of lipopolysaccharide (LPS) and cecal ligation/perforation (CLP)-induced sepsis-related acute kidney injury .
FPR2 agonist 3 (compound CMC23) can limit the lactate dehydrogenase release in LPS (HY-D1056) -stimulated cultures and decrease the levels of pro-inflammatory IL-1β and IL-6. FPR2 agonist 3 decrease the level of phosphor-STAT3 via the STAT3/SOCS3 signaling pathway .
NF-κB-IN-14 (compound 5e) significantly inhibits nitric oxide production in LPS-induced macrophages (IC50: 6.4 μM). NF-κB-IN-14 disrupts the TLR4-MyD88 protein interaction, leading to the suppression of the NF-κB signaling pathway suppression. NF-κB-IN-14 reduces ear edema and inflammation in an atopic dermatitis mouse model .
S-HP210 is a potent and selective glucocorticoid receptor (GR) with an IC50 value of 1.92 μM for NF-κB transrepression (TR). S-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. S-HP210 is nontoxic at effective doses against mouse fibroblasts 3T3 cells .
NF-κB-IN-10 (compound E1) is an NF-κB inhibitor that can improve heart failure by reducing oxidative stress and inflammation by regulating Nrf2/NF-κB signaling pathway. NF-κB-IN-10 inhibits LPS-induced NO production and expression of iNOS and COX-2 in RAW264.7 cells. NF-κB-IN-10 can be used in the research of cardiovascular diseases .
COX-2/15-LOX-IN-3 (compound 5k) is a dual inhibitor of COX-2/15-LOX with IC50s of 0.075 μM and 1.97 μM, respectively. COX-2/15-LOX-IN-3 can inhibit LPS-induced cell production of promoting cytokines (IL-6, ROS, and NO), with specific anti-inflammatory activity .
COX-2/15-LOX-IN-4 (compound 5i) is a dual inhibitor of COX-2/15-LOX with IC50s of 0.075 μM and 1.97 μM, respectively. COX-2/15-LOX-IN-4 can inhibit LPS-induced cell production of promoting cytokines (IL-6, ROS) with specific anti-inflammatory activity .
(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsin B inhibitor. (S,S)-Z-FA-FMK blocks LPS-induced production of IL-1α and IL-1β. (S,S)-Z-FA-FMK can be used as a negative control for caspase-1 and caspase-2 inhibitors because it lacks an aspartic acid residue at the P1 position .
Articaine (hydrochloride) (Standard) is the analytical standard of Articaine (hydrochloride). This product is intended for research and analytical applications. Articaine hydrochloride (Hoe-045) is an amide anaesthetic containing an ester group, reversibly binding to the α-subunit of the voltage-gated sodium channels within the inner cavity of the nerve, can provide effective pain relief. Articaine hydrochloride ameliorates LPS-induced acute kidney injury via inhibition of NF-ĸB activation and the NLRP3 inflammasome pathway .
TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR .
DHQZ 36 is a potent inhibitor of retrograde trafficking. DHQZ 36 inhibits Leishmania amazonensis infection in macrophages with an EC50 of 13.63 μM. DHQZ 36 has potent anti-parasite activity .
VRT-043198, the agent metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively .
15-LOX-1 inhibitor 1 is a potent inhibitor of 15-LOX-1 (15-lipoxygenase-1) with an IC50 value of 0.19 μM. 15-LOX-1 inhibitor 1 protects macrophages from lipopolysaccharide-induced cytotoxicity. 15-LOX-1 inhibitor 1 inhibits NO formation and lipid peroxidation .
IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC50 values of 3.53 μM (IDO1) and 1.15 μM (TDO). IDO1/TDO-IN-4 forms hydrogen bond with IDO1, and π−π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression, and depression-induced infectious, metabolic, and autoimmune disorders .
PF-184 is a potent and selective IKK-2 inhibitor (IC50: 37 nM) over rhIKK-1, IKKi, and more than 30 tyrosine and serine/threonine kinases. PF-184 can be used in the research of inflammation, such as asthma and chronic obstructive pulmonary disease .
2'-Fucosyllactose (2'-FL) is an oligosaccharide that could be derived from human milk. 2'-Fucosyllactose regulates the expression of CD14, alleviates colitis and regulates the gut microbiome. 2'-Fucosyllactose stimulates T cells to increase IFN-γ production and decreases IL-6, IL-17, and TNF-α production of cytokines .
NLRP3-IN-14 is a potent and selective NLRP3 inflammasome inhibitor (KD: 5.87 μM). NLRP3-IN-14 inhibits IL-1β release with an IC50 of 0.131 μM. NLRP3-IN-14 can be used for the research of inflammation .
NLRP3-IN-15 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-15 inhibits IL-1β release with an IC50 of 0.114 μM. NLRP3-IN-15 can be used for the research of inflammation .
NLRP3-IN-16 is a potent and selective NLRP3 inflammasome inhibitor. NLRP3-IN-16 inhibits IL-1β release with an IC50 of 0.065 μM. NLRP3-IN-16 can be used for the research of inflammation .
Ac2-26 ammonium is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 ammonium induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ammonium ameliorates lung ischemia-reperfusion injury. Ac2-26 ammonium also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
Belnacasan (VX-765) is an orally bioactive proagent of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM .
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. .
PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease) .
MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively .
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone), a flavonoid compound, possesses potent anti-inflammatory effects in LPS-induced macrophage cell line mediated by inhibition of release of inflammatory mediators, NO, PGE2, and pro-inflammatory cytokines. 7,3',4'-Tri-O-methylluteolin significantly induces reduction in the mRNA expressions of inducible nitric oxide synthase and cyclooxygenase-2 .
Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway .
Santamarine (Santamarin), a sesquiterpene lactone, increases HO-1 expression through Nrf2 translocation and suppresses NO, PGE2, TNF-α, and IL-1β production through inhibition of NF-κB translocation in LPS-induced macrophages. Santamarine shows anti-photoaging properties via inhibition of MAPK/AP-1 and stimulation of TGF-β/Smad signaling in UVA-irradiated human dermal fibroblasts (HDFs). Antioxidant activities .
NADPH oxidase-IN-1 is an orally active NADPH oxidase (Nox) inhibitor, related with neuronal inflammation. NADPH oxidase-IN-1 can cross the blood-brain barrier (BBB), inhibits Nox2 and Nox4 with IC50s of 1.9 μM and 2.47 μM, respectively. NADPH oxidase-IN-1 suppresses pro-inflammatory cytokines production and LPS-mediated microglial migration, also has in vivo efficacy .
Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue with anti-inflammatory activity. Anti-inflammatory agent 35 blocks mitogen-activated protein kinase (MAPK) signaling and p65 nuclear translocation of NF-kB. Anti-inflammatory agent 35 also inhibits yellow neutrophil infiltration and pro-inflammatory cytokine production. Anti-inflammatory agent 35 significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI) in vivo .
JNK2-IN-1 (Compound J27) is a JNK2 inhibitor (Kds: 79.2 μM). JNK2-IN-1 has anti-inflammatory activity. JNK2-IN-1 decreases the release of TNF-α and IL-6 through inhibiting the activation of NF-κB/MAPK pathway. JNK2-IN-1 alleviates the symptoms of LPS-induced acute lung injury (ALI) and sepsis .
HDAC6-IN-34 (compound 21) is an oral active and selective HDAC6 inhibitor with the IC50 of 18 nM. HDAC6-IN-34 increases the acetylation level of tubulin without affecting histone acetylation in cutaneous T-cell lymphoma cells and inhibits TNF-α secretion in LPS (HY-D1056)-stimulated macrophage cells. HDAC6-IN-34 shows excellent anti-arthritic efficacy in rat .
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta .
Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models , has selective inhibitory activity towards cyclooxygenase-2 (COX-2) .
Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways .
Tau-aggregation and neuroinflammation-IN-1 is a potent tau-aggregation and neuroinflammation inhibitor. Tau-aggregation and neuroinflammation-IN-1 exhibits remarkable inhibitory activities against AcPHF6 and full-length tau aggregation. Tau-aggregation and neuroinflammation-IN-1 has a low cytotoxicity and reduced NO release in LPS-stimulated BV2 cells. Tau-aggregation and neuroinflammation-IN-1 can reverse okadaic acid-induced memory impairment in rats .
Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibits JNK and p38MAPK signals. Lucidone also has inhibitory activity against Dengue virus (DENV) (EC50=25 μM) .
16:0 PEG350 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
16:0 PEG550 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
16:0 PEG750 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG350 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG550 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG750 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
16:0 PEG1000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
16:0 PEG3000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
16:0 PEG5000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG1000 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG3000 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG5000 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG350 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG550 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG750 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG1000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG3000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG5000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:1 PEG350 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:1 PEG550 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:1 PEG1000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:1 PEG3000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:1 PEG5000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
Anti-inflammatory agent 54 (compound 9c) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 2.4 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model .
Anti-inflammatory agent 55 (compound 9j) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 0.8 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model .
Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment .
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases .
Ethyl ferulate, a naturally lipophilic derivative of ferulic acid originally derived from Rhizoma Chuanxiong, induces heme oxygenase-1 (HO-1) and protects rat neurons against oxidative stress . Ethyl ferulate also protects neurons against amyloid β peptide (1-42)-induced oxidative stress and neurotoxicity .
Soyasapogenol B is a component of soy that has oral activity. Soyasapogenol B promotes autophagy and apoptosis. Soyasapogenol B has anti-inflammatory, antioxidant and antitumor activities .
VUF11207 fumarate is a CXCR7 agonist that binds specifically to CXCR7. VUF11207 fumarate reduces CXCL12-mediated osteoclastogenesis and bone resorption by inhibiting ERK phosphorylation .
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels .
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10 .
Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC50 of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells .
Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .
Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects .
AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis .
JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively . Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607 .
4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR)TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model .
Narchinol B (Compound 4) is a sesquiter penoid
compound. Narchinol B has anti-inflammatory effects. Narchinol B works by
inhibiting proinflammatory mediators, including prostaglandin E2 (PGE2),
inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) proteins,
as well as proinflammatory cytokines, such as interleukin-1b, IL-6, and tumor
necrosis factor-α (TNF-α). Narchinol B significantly inhibits LPS-induced
overproduction of NO in BV2 cells (IC50=2.43 μM)
.
Lactoferrin 17-41 (Lactoferricin B), a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 has antitumor activities .
KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury .
FW1256 is a phenyl analogue and a slow-releasing hydrogen sulfide (H2S) donor. FW1256 inhibits NF-κB activity and induces cell apoptosis. FW1256 exerts potent anti-inflammatory effects and has the potential for cancer and cardiovascular disease treatment .
Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor .
Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 acetate has antitumor activities .
PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation .
FPR2 agonist 2 is a potent and permeates the blood−brain barrier FPR2 agonist with an EC50 of 0.13 µM, 1.1 µM for FPR2 and FPR1, respectively. FPR2 agonist 2 inhibits the production of pro-inflammatory cytokines, counterbalances the changes in mitochondrial function, and inhibits caspase-3 activity .
(Rac)-PF-184 hydrate is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. (Rac)-PF-184 hydrate has anti-inflammatory effects .
TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor with a KD value of 12.06 μM. TNF-α-IN-11 binds to TNF-α and blocks the activation of TNF-α-trigged caspase and NF-κB signaling pathway. TNF-α-IN-11 inhibits the phosphorylation of IκBα, as well as the nuclear translocation of NF κB p65. TNF-α-IN-11 can be used for research of TNF-α-mediated autoimmune diseases .
2,4,6-Trichlorol-3-methyl-5-methoxy-phenol 1-O-β-d-glucopyranosyl-(1 → 6)-β-d-glucopyranoside is a chlorophenyl glycoside found in the bulbs of Lilium brownie var. viridulum. 2,4,6-Trichlorol-3-methyl-5-methoxy-phenol 1-O-β-d-glucopyranosyl-(1 → 6)-β-d-glucopyranoside exhibits weak inhibition of NO production in LPS-stimulated RAW 264.7 cells .
NLRP3/AIM2-IN-3 (compound 59) is a potent inhibitor with differential species specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis. NLRP3/AIM2-IN-3 shows inhibitory efficacy against pyroptosis in THP-1 macrophages stimulated with LPS/nigericin, with an IC50 of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 disturbs the interaction of NLRP3 or AIM2 with the adaptor protein ASC and inhibited ASC oligomerization .
Anti-Aβ agent 1A (compound M15) has potent activity against amyloid-β. Anti-Aβ agent 1A possesses can significantly inhibit LPS-induced levels of IL-1β, IL-6 and TNF-α, and reduces the apoptosis of SH-SY5Y induced by H2O2 through mitochondria pathway. Anti-Aβ agent 1A possesses antioxidant, anti-inflammatory, anti-Aβ toxicity and neuroprotective activities. Anti-Aβ agent 1A can be used for researching Alzheimer’s disease (AD) .
PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC50 of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β, IL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al .
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1 .
1,3,5-Trihydroxy-4-prenylxanthone is a Na +/H + exchange system (Na+/H+ Exchanger (NHE)) inhibitor with a minimum inhibitory concentration of 10 μg/mL . 1,3,5-Trihydroxy-4-prenylxanthone is a phosphodiesterase type 5 (PDE5) (Phosphodiesterase (PDE)) inhibitor with an IC50 value of 3.0 μM . 1,3,5-Trihydroxy-4-prenylxanthone inhibits Lipopolysaccharide (LPS) (Lipopolysaccharides (HY-D1056))-induced NO production in RAW264.7 macrophages, and has anti-inflammatory activities .
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
Tizoxanide (Standard) is the analytical standard of Tizoxanide. This product is intended for research and analytical applications. Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC50 of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells .
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
(R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is a lysophosphatidic acid acyltransferase inhibitor with an IC50 of 0.6 µM and interrupts IL-12 signaling-mediated STAT4 activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research .
EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo. EHT 1864 dependently suppresses the release of migrasomes from podocytes induced by LPS, PAN, or HG .
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1 . GSK-J4 induces endoplasmic reticulum stress-related apoptosis .
Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties . Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways . Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM .
(3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid, a lanostane triterpenoids, exhibits obvious NO inhibitory activity on n LPS-induced BV-2 microglia cells with an IC50 of 9.55 uM. (3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid has anti-inflammatory activities .
α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
Avicularin is an orally active flavonoid. Avicularin inhibits NF-κB (p65), COX-2 and PPAR-γ activities. Avicularin has anti-inflammatory, anti-infectious anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities .
N-Salicyloyltryptamine acts on voltage-dependent Na +, Ca 2+, and K + ion channels inhibitor. N-Salicyloyltryptamine inhibits K + currents with an IC50 value of 34.6 μM (Ito). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect - .
BODIPY TR Cadaverine, a cadaverine derivative, is a red fluorescent dye. BODIPY TR Cadaverine can be used in a a highly sensitive and robust fluorescent displacement assay, which binds to native LPS strongly, specifically recognizing lipid A, and is competitively displaced by compounds displaying an affinity for lipid A .
Sunset Yellow FCF (Orange Yellow S) is an orange azo dye with a maximum absorption wavelength of 480 nm. Sunset Yellow FCF can be used in food, cosmetics and pharmaceuticals .
Lipopolysaccharides (LPS) is an endotoxin derived from the outer leaflet of the outer membrane of Gram-negative bacteria. Lipopolysaccharides consists of an antigen O-specific chain, a core oligosaccharide and lipid A. Lipopolysaccharides is a pathogenic associated molecular pattern (PAMP) that activates the immune system. Lipopolysaccharides activates TLR-4 on immune cells . This product is derived from Escherichia coli O55:B5. Lipopolysaccharides induces secretion of cell migrasome .
16:0 PEG350 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
16:0 PEG550 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
16:0 PEG750 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG350 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG550 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG750 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
16:0 PEG1000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
16:0 PEG3000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
16:0 PEG5000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG1000 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG3000 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:0 mPEG5000 PE (ammonium) is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG350 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG550 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG750 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymeric nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG1000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG3000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
14:0 PEG5000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:1 PEG350 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:1 PEG550 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:1 PEG1000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:1 PEG3000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
18:1 PEG5000 PE is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles. Through biotin modification and carboxyl terminus, lipid nanoparticles (LNPs) further coupling with other biomolecules can be achieved. Functionalized nanoparticles can be used for targeted labeling of specific cellular proteins. With streptavidin as a linker, biotinylated PEG lipid-conjugated polymer nanoparticles are able to bind to biotinylated antibodies on cell surface receptors, yielding the utility of fluorescence-based imaging and sensing.
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
Endotoxin inhibitor TFA is a synthetic peptide that binds lipid A with high affinity, thereby detoxifying LPS (HY-D1056) and preventing LPS-induced cytokine release in vivo. Endotoxin inhibitor TFA inhibits the febrile response to LPS with very low toxicity and lethality .
RS09 is a LPS peptide mimic serves as a candidate to be considered as a new class of TLR4 agonist adjuvant. RS09 increases antibody production in a vaccine setting .
Pep19-2.5 is an synthetic and antitoxin peptide, blocks the intracellular endotoxin signaling cascade. Pep19-2.5 inhibits signaling of lipopeptides (LP) and lipopolysaccharides (LPS) mediated by transmembrane and cytosolic pattern recognition receptors (PRRs). The signaling cascades lead to inflammation and cell pyroptosis .
Endotoxin inhibitor a synthetic peptide that binds lipid A with high affinity, thereby detoxifying LPS (HY-D1056) and preventing LPS-induced cytokine release in vivo. Endotoxin inhibitor inhibits the febrile response to LPS with very low toxicity and lethality .
Citrullinated LL-37 5cit is a citrullinated LL-37 (HY-P1222) peptide. The antiviral and antibacterial effects of Citrullinated LL-37 5cit are significantly reduced compared to native LL-37. Citrullinated LL-37 5cit is unable to reduce LPS-mediated release of TNF-α due to a lack of LPS-binding capacity .
Diplacol ia a natural compound from from Mimulus clevelandi and shows potent inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide production .
SpHistin is an antimicrobial peptide (AMP). SpHistin can bind to LPS (HY-D1056) and permeabilize the bacterial membrane. SpHistin combined with Rifampicin (HY-B0272) and Azithromycin (HY-17506) promotes the intracellular uptake of the antibiotics and subsequently enhances the bactericidal activity of both agents against P. aeruginosa .
Tiprelestat is a potent human neutrophil elastase inhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease .
Ac2-26 ammonium is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 ammonium induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ammonium ameliorates lung ischemia-reperfusion injury. Ac2-26 ammonium also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
Lactoferrin 17-41 (Lactoferricin B), a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 has antitumor activities .
Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 acetate has antitumor activities .
Polymixin B is a mixture of B1 and B2 polypeptides obtained from different strains of Bacillus polymyxa, with antibacterial activity against gram-negative bacteria. It can bind lipopolysaccharide (LPS) of the outer membrane of gram-negative bacteria and disrupts the cytoplasmic membrane by inducing large pores to allow nucleotide leakage in bacterial walls. This disrupts the permeability of the cytoplasmic membrane.
Panobacumab (KBPA101) is a fully human IgM/κ monoclonal antibody generated by immortalizing human B lymphocytes against the LPS O polysaccharide of serotype O11 of P. aeruginosa .
Atibuclimab, is a chimeric monoclonal antibody directed against CD14 and is composed of murine variable and human IgG4 Fc regions. Atibuclimab can be used for the research of amyotrophic lateral sclerosis . Atibuclimab attenuates LPS-induced symptoms and strongly inhibits LPS-induced proinflammatory cytokine release, while only delaying the release of the anti-inflammatory cytokines soluble TNF receptor type I and IL-1 receptor antagonist .
Lipopolysaccharides (LPS) is an endotoxin derived from the outer leaflet of the outer membrane of Gram-negative bacteria. Lipopolysaccharides consists of an antigen O-specific chain, a core oligosaccharide and lipid A. Lipopolysaccharides is a pathogenic associated molecular pattern (PAMP) that activates the immune system. Lipopolysaccharides activates TLR-4 on immune cells . This product is derived from Escherichia coli O55:B5. Lipopolysaccharides induces secretion of cell migrasome .
Vogeloside is an iridoid that can be isolated from the roots of Triosteum pinnatifidum. Vogeloside inhibits nitric oxide production in LPS-activated macrophages .
Bullatantriol ((+)?-?Bullatantriol) can be isolated from the roots of Homalomena aromatica. Bullatantriol can promote the proliferation and differentiation of osteoblasts. Bullatantriol also inhibits LPS-induced NO production in BV2 cells .
Moracin C, a natural product, is an anti-inflammatory agent. Moracin C inhibits LPS-activated reactive oxygen species (ROS) and nitric oxide (NO) release from cells .
Deoxyandrographolide suppresses LPS induced increase in mRNA levels of iNOS as well as production of proinflammatory mediators TNF-α and IL-6. Deoxyandrographolide potentiates NGF-induced neurite outgrowth .
Berkeleyacetal C, a meroterpenoid compound, shows favorable activity of inhibiting nitrogen oxide (NO) production of macrophages stimulated by lipopolysaccharide (LPS). Berkeleyacetal C exerts anti-inflammatory effects via inhibiting NF-κB, ERK1/2 and IRF3 signaling pathways .
(4S)-10-Nor-calamenen-10-one (Compound 15) enhances LPS-induced NO production by microglia. (4S)-10-Nor-calamenen-10-one is an eudesmane sesquiterpene that can be isolated from Alpinia oxyphylla .
Loganic acid 6′-O-β-D-glucoside, a iridoidal glucoside, is isolated from the whole plant of Gentiana rhodantha (Gentianaceae). Loganic acid 6′-O-β-D-glucoside inhibits LPS-induced NO and TNF-α production in macrophage RAW264.7 cells .
Hedycoronen A has inhibitory activity on the IL-6, IL-12 p40, and TNF-α production in LPS-Stimulated BMDCs, with IC50s of 9.1 μM, 5.6 μM, and 46.0 μM. Hedycoronen A can be isolated from Hedychium coronarium .
Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity .
(6E)-1,7-Bis(4-hydroxyphenyl)-6-hepten-3-one (compound7) is a nature product isolated from rhizomes of Curcuma kwangsiensis. (6E)-1,7-Bis(4-hydroxyphenyl)-6-hepten-3-one has inhibitory effect on NO production induced by LPS in macrophages with an IC50 value of 8.93 μM .
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation .
Catalpalactone has anti-inflammatory effect. Catalpalactone inhibits LPS-induced NO production and iNOS expression in RAW264.7 cells, and also inhibits IRF3, NF-κB, and IFN-β/STAT-1 activation. Catalpalactone also inhibits dopamine biosynthesis by reducing tyrosine hydroxylase (TH) and aromatic-l-amino acid decarboxylase (AADC) activities .
Delphinidin-3-sambubioside (Dp3‐Sam) chloride is an anthocyanin that has orally active anti-inflammatory activity. Delphinidin-3-sambubioside chloride inhibits LPS-induced inflammatory factors release. Delphinidin-3-sambubioside chloride also alleviates hepatic lipid accumulation in HFD rats. Delphinidin-3-sambubioside chloride can be isolated from Hibiscus sabdariffa L. .
Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction .
1-Dehydro-[10]-gingerdione directly inhibits IKKβ activity by targeting the activation loop of IKKβ, thus disrupting IKKβ-catalysed IκBα phosphorylation in macrophages stimulated with agonists. 1-Dehydro-[10]-gingerdione inhibits LPS (HY-D1056)-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione has the potential for NF-κB-associated inflammation and autoimmune disorders research .
Kdo2-Lipid A ammonium is a chemically defined lipopolysaccharide (LPS) with endotoxin activity equal to LPS. Kdo2-Lipid A ammonium is highly selective for TLR4. Kdo2-Lipid A ammonium stimulates the release of both TNF and PGE2 .
Isogosferol ((+)-Isogospherol; Isogospherol) is a potent anti-inflammatory agent. Isogosferol decreases LPS (HY-D1056)-stimulated NO and IL-1β expression. Isogosferol decreases the LPS (HY-D1056)-stimulated expression of iNOS, COX-2, NF-κB, and pERK1/2 .
Taxamairin B is a potent anti-inflammatory agent. Taxamairin B decreases proinflammatory cytokines (TNF-α, IL-1β and IL-6) expression and the production of NO and ROS in LPS-induced RAW264.7 cells. Taxamairin B exhibits significant
protective effects in LPS-induced acute lung injury in mice .
20-Hydroxyganoderic Acid G is a lanostane triterpenoid obtained from the EtOH extract of fruiting bodies of the Ganoderma curtisii. 20-Hydroxyganoderic Acid G inhibits BV-2 microglia cells activated by LPS with an IC50 of 21.33 μM. 20-Hydroxyganoderic Acid G has therapeutic potential in the agent discovery of nerve inflammation diseases associated with microglia activated by LPS .
Chitohexaose hexahydrochloride is a chitosan oligosaccharide with anti-inflammatory effect. Chitohexaose hexahydrochloride binds to the active sites of TLR4 and inhibits LPS induced inflammation .
Isomaculosidine is an alkaloid that can be isolated from D. dasycarpus. Isomaculosidine can inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated BV2 microglial cells .
O-Acetylschisantherin L (Acetylschisantherin L) is a natural lignan, which exhibits inhibitory effects on LPS-induced NO production in BV-2 cells with an IC50 of 23.1 μM .
Anhydronotoptol is a potent nitric oxide inhibitory coumarin. Anhydronotoptol inhibits NO production in RAW 264.7 cells induced by LPS with an IC50 value of 36.6 μM .
Lonicerin is an anti-algE (alginate secretion protein) flavonoid with inhibitory activity for P. aeruginosa. Lonicerin prevents inflammation and apoptosis in LPS-induced acute lung injury .
(3β,24S)-3-Hydroxystigmast-5-en-7-one (Compound 31) is a compound that can be isolated from Lindera akoensis . (3β,24S)-3-Hydroxystigmast-5-en-7-one has anti-inflammatory activity .
Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways .
Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity .
Herpotrichone A shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.41 μM.
Curindolizine, indolizine alkaloid , displays an anti-inflammatory action in lipopolyssacharide (LPS)-induced RAW 264.7 macrophages with an IC50 value of 5.31 μM .
Hyuganin D (Isobocconin) is a Coumarin (HY-N0709) constituent that substantially inhibits LPS (HY-D1056)-induced NO production in mouse peritoneal macrophages .
Neocurdione is a hepatoprotective sesquiterpene isolated from Curcuma zedoaria rhizome. Neocurdione exerts potent effect on D-galactosamine- (D-Gain) and lipopolysaccharide- (LPS) induced acute liver injury in mice .
3-O-Acetyl-16α-hydroxydehydrotrametenolic acid, an anti-inflammatory triterpenoid, inhibits NO production and iNOS expression in LPS-stimulated Raw264.7 cells .
Herpotrichone B shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.11 μM.
Chloranthalactone E (compound 6), a labdane diterpene, can be isolated from the aerial parts of Chloranthus serratus. Chloranthalactone E inhibits NO production in LPS-activated RAW 264.7 macrophages .
Vitexdoin A is a nitric oxide scavenging lignin. Vitexdoin A inhibits NO production with an IC50 of 0.38 μM in LPS (HY-D1056)-stimulated RAW 264.7 cells .
12-Dehydrogingerdione is an inhibitor of NO Synthase. 12-Dehydrogingerdione signi?cantly inhibits LPS-stimulated production of NO, IL-6 and PGE2 in Raw 264.7 cells .
Isomucronulatol is a flavonoid isolated from the roots of A. membranaceus. Isomucronulatol exhibits inhibitory effects on LPS-stimulated production IL-12 p40 in vitro and has potential anti-inflammatory effect .
Inflexuside B, an abietane diterpenoid, can be isolated from the aerial parts of Isodon inflexus. Inflexuside B strongly inhibits lipopolysaccharide (LPS)-activated NO Synthase in RAW264.7 macrophages .
Inflexuside A, an abietane diterpenoid, can be isolated from the aerial parts of Isodon inflexus. Inflexuside B strongly inhibits lipopolysaccharide (LPS)-activated NO production (NO Synthase) in RAW264.7 macrophages .
Phaeocaulisin E (Compound 5) is a guaiane-type sesquiterpene that inhibits LPS HY-(HY-D1056)-induced NO production in RAW 264.7 macrophages with an IC50 of 10.3 μM .
Kanshone B (Compound 5) is isolated from the
natural Nardostachys chinensis. Kanshone B shows inhibitory
activity against LPS-induced NO production (IC50=11.5 μM)
.
Epimagnolin B is a bisepoxylignan isolated from Magnolia fargesii, with anti-inflammatory activity and antiallergic effects. Epimagnolin B inhibits NO production in LPS-activated microglia. Epimagnolin B exhibited antiallergic effects .
Licoagrochalcone C, a flavonoid, reveals efficacious inhibitory activity on NF-κB transcription. Licoagrochalcone C shows significant inhibitory activity on LPS (HY-D1056)-induced NO production .
9-Hydroxy-α-lapachone (α-Dihydrocaryopterone) is a natural phenol, exhibits potent inhibitory effects with an IC50 of 4.64 µM on LPS-induced NO production in RAW 264.7 cells .
N-cis-Feruloyl tyramine (cis-N-(4-Hydroxyphenethyl) ferulamide) is a natural phenolic compound, exhibits modest inhibitory activity on LPS-activated NO production in RAW 264.7 cells .
Inubritannolide A displays slight strong neuroprotective potency against different types of neuronal cells mediated by various inducers including H2O2, 6-hydroxydopamine (6-OHDA), and lipopolysaccharide (LPS).
Sibiricine (Compound 8) is an isoquinoline alkaloid derived from the medicinal plant Corydalis crispa. Sibiricine has significant anti-inflammatory activity on TNF-α production by LPS-activated THP-1 cells .
Plantamajoside is a phenylpropanoid glycoside isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside has protective effects on LPS-induced acute lung injury (ALI) mice model. Plantamajoside has the potential for the treatment of pulmonary inflammation .
Dehydroandrographolide can be extracted from herbal medicine Andrographis paniculata Nees. Dehydroandrographolide reduces oxidative stress in LPS-induced acute lung injury by inactivating iNOS. Dehydroandrographolide has anti-infective activity .
Hyperelamine A (compound 5) is a polycyclic polyprenylated acylphloroglucinols (PPAPs). Hyperelamine A exhibits inhibitory activity against LPS-activated NO production in BV-2 cells via TLR-4/NF κB signaling .
Guaiacol (Standard) is the analytical standard of Guaiacol. This product is intended for research and analytical applications. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation . Anti-inflammatory activity .
15a-Hydroxy-3,11,23-trioxo-lanost-8,20-dien-26-oic acid, a Lanostane triterpenoid, possesses NO production inhibitory activities of LPS-induced microglia .
Geranylgeraniol is an orally acitve vitamin K2 sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model .
NF-κB-IN-13 (compound 12) can significantly inhibit LPS-induced NF-κB activation and NO production in RAW264.7 macrophages. NF-κB-IN-13 has anti-inflammatory effects .
Saucerneol is a lignans that can be isolated from Saururus chinensis. Saucerneol inhibits LPS-induced or Con A-induced lymphocytes proliferation. Saucerneol inhibits mixed lymphocyte response. Saucerneol also inhibits mitogens-induced cytokines secretion .
Isodorsmanin A is an anti-inflammatory agent. Isodorsmanin A suppresses the production of inflammatory mediators and proinflammatory cytokines. Isodorsmanin A inhibits the phosphorylation of JNK, MAPK .
Esculentic acid is a selective COX-2 inhibitor and has anti-inflammatory effect. Esculentic acid is a pentacyclic triterpenoid that can be extracted from the Chinese herb Phytolacca esculenta .
Damnacanthol is a natural product that can be isolated from Damnacanthus major . Damnacanthol has anti-15-lipoxygenase activity and can inhibit nitric oxide production in LPS-activated macrophages RAW 264.7 cells .
(Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation .
8-Methylsulfinyloctyl isothiocyanate, an isothiocyanate, has antimicrobial activity and remarkable inhibitory activity against plant growth . 8-Methylsulfinyloctyl isothiocyanate impair COX-2 mediated inflammatory responses in LPS stimulated raw macrophages .
Chebulanin, a polyphenol acid, exerts its anti-inflammatory and anti-arthritic effects via inhibiting NF-κB and MAPK activation in collagen-induced arthritis mice. Chebulanin inhibits the nuclear translocation of p38 and p65 in LPS-stimulated macrophages .
Inulicin (1-O-Acetylbritannilactone) is an active compound that inhibits VEGF-mediated activation of Src and FAK. Inulicin (1-O-Acetylbritannilactone) inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
Bisabolangelone, a sesquiterpene derivative, is isolated from the roots of Osterici Radix. Bisabolangelone possesses anti-inflammatory properties, which inhibits LPS-stimulated inflammation through the blocking of NF-kappaB and MAPK pathways in macrophages. Bisabolangelone has anti-ulcer activities .
α-Glucosidase-IN-37 (Compound 11) moderately inhibits LPS-induced NO production with an IC50 value of 23.7 μM in macrophages. α-Glucosidase-IN-37 has weak inhibitory activity against α-Glucosidase .
Diplacol is a geranylated flavanone that can be isolated from paulownia trees (Paulownia coreana UYEKI). Diplacol has anti-inflammatory activity. Diplacol inhibits NO production in LPS-stimulated Raw264.7 cells with an IC50 value of 4.53 μM .
Asperbisabolane L, a sesquiterpenoid, exerts the anti-inflammatory activity by inhibiting the NF-κB-activated pathway. Asperbisabolane L inhibits the translocation of NF-κB from cytoplasm to the nucleus. Asperbisabolane L also inhibits NO production in LPS-activated BV-2 microglia cells .
Pratol is a potent inhibitor of NF-κB. Pratol significantly reduces NO and prostaglandin PGE2 production without any cytotoxic in LPS-stimulated RAW 264.7 cells. Pratol reduces proinflammatory cytokines. Pratol can be used in study inflammatory diseases and cancer .
Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 inhibits VCAM-1 and ICAM-1 expressions stimulated with lipopolysaccharide (LPS). Ginsenoside Rg2 also reduces Aβ1-42 accumulation.
Isomucronulatol 7-O-glucoside is a flavonoid isolated from the roots of A. membranaceus. Isomucronulatol 7-O-glucoside exhibits weak inhibitory effects on LPS-stimulated production IL-12 p40 in vitro and has potential anti-inflammatory effect .
Shegansu B is an inhibitor of IL-1β. Shegansu B 6 inhibits IL-1β expression on LPS-induced THP-1 cells with 64.74% inhibition. Shegansu B has anti-inflammatory activity .
13-Methylberberine chloride (13-Methylberberinium chloride), a berberine analogue, has anti-adipogenic and antitumor activities. 13-Methylberberine chloride (13-Methylberberinium chloride) increases production of IL-12 and inhibits the expression of iNOS at posttranscriptional level in macrophages activated with LPS .
Methyl everninate is the major constituent of the deuterochloroform. Methyl everninate, rhodomollosides A and B are the derivatives of Methyl everninate, with cytotoxicity against RAW264.7 cells. Both of they shows inhibitory effects with a lipopolysaccharide (LPS)-stimulated murine macrophages RAW 264.7 cells model .
Absinthin is a structurally unique triterpene, and is responsible for the high bitter value of wormwood. Absinthin is an agonist of the bitter taste receptor hTAS2R46, which reduces cytosolic Ca 2+-rises induced by histamine by a receptor-specific mechanism mediated by hTAS2R46 .
25S-Inokosterone is a phytoecdysone in the roots of two same species of A. bidentata Blume and A. japonica Nakai, and two different species of C. capitata Moq and C. officinalis Kuan. 25S-Inokosterone has the potential for the LPS-induced acute kidney injury research .
Apiin, a major constituent of Apium graveolens leaves with anti-inflammatory properties. Apiin shows significant inhibitory activity on nitrite (NO) production (IC50 = 0.08 mg/mL) in-vitro and iNOS expression (IC50 = 0.049 mg/ mL) in LPS-activated J774.A1 cells .
Kauran-16,17-diol (ent-Kauran-16β,17-diol), a natural diterpene, posseses anti-tumor and inducing-apoptosis activity, with a IC50 of 17 μM on inhibiting NO production in LPS-stimulated RAW 264.7 macrophages .
Isoforskolin is the principle active component of C. forskohlii native to China. Isoforskolin reduces the secretion of lipopolysaccharide (LPS)-induced cytokines, namely TNF-α, IL-1β, IL-6 and IL-8, in human mononuclear leukocytes. Isoforskolin acts as an anti-inflammatory agent for the treatment of Lyme arthritis .
Sanggenon A (Sanggenone A) exerts anti-inflammatory effects by regulating NF-κB and HO-1/Nrf2 signaling pathways in BV2 and RAW264.7 cells. Sanggenon A markedly inhibits the Lipopolysaccharide (LPS; HY-D1056)-induced production of nitric oxide .
Nyasol ((-)-Nyasol) is an active compound that has antifungal, antibacterial, antileishmanial, hyaluronidase inhibition activities. Nyasol inhibits LTB4 binding to human neutrophils. Nyasol suppresses neuroinflammatory response through the inhibition of I-κB degradation in LPS (HY-D1056)-stimulated BV-2 microglial cells .
7-Deacetylgedunin is an activator of Keap1/Nrf2/HO-1. 7-Deacetylgedunin alleviates mice mortality induced by LPS. 7-Deacetylgedunin inhibits Keap1 expression and suppresses macrophage proliferation. 7-Deacetylgedunin suppresses inflammation in vivo and in vitro .
Cavidine ((+)-Cavidine) is a selective COX-2 inhibitor which possesses anti-inflammatory activity. Cavidine can be used for the research of skin injuries, hepatitis, cholecystitis, and scabies. Cavidine ameliorates LPS (HY-D1056)-induced acute lung injury via NF-κB signaling pathway .
Ruscogenin suppresses HCC metastasis by reducing the expression of MMP-2, MMP-9, uPA, VEGF and HIF-1α via regulating the PI3K/Akt/mTOR signaling pathway . And Ruscogenin alleviates LPS-induced pulmonary endothelial cell apoptosis by su
Cimifugin (Cimitin) is a bioactive component of Cimicifuga racemosa, a Chinese herb. Cimifugin suppresses allergic inflammation by reducing epithelial derived initiative key factors via regulating tight junctions . Cimifugin reduces the migration and chemotaxis of RAW264.7 cells and inhibits the release of inflammatory factors and activation of MAPKs and NF-κB signaling pathways induced by LPS .
6-Hydroxyflavone is a naturally occurring flavone, with anti-inflammatory activity. 6-Hydroxyflavone exhibits inhibitory effect towards bovine hemoglobin (BHb) glycation. 6-Hydroxyflavone can activate AKT, ERK 1/2, and JNK signaling pathways to effectively promote osteoblastic differentiation. 6-Hydroxyflavone inhibits the LPS-induced NO production .
α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects .
Vitisin A has antioxidative, anticancer, antiapoptotic, neuroprotective and anti-inflammatory effects. Vitisin A inhibits LPS-induced NO and iNOS production via down-regulation of ERK1/2 and p38 and the NF-κB signal pathway. Vitisin A also inhibits adipocyte differentiation. Vitisin A is a resveratrol tetramer that can be isolated from Vitis vinifera roots .
Sarglaroids F (compound 6) is an anti-inflammatory agent isolated from the roots of Grass Coral. Sarglaroids F inhibits LPS/ATP-induced IL-1β release by affecting K+ efflux and reducing Caspase-1(P20) levels. Sarglaroids F is not cytotoxic to RAW264.7 cells .
Bis-5,5-Nortrachelogenin is isolated from active extract of root of Wikstroemia indica. Bis-5,5-Nortrachelogenin inhibits nitric oxide (NO) production in a lipopolysaccharide (LPS) and recombinant mouse interferon-γ(IFN-γ) activated murine macrophage-like cell line, RAW 264.7 with an IC50 value of 48.6 mM .
Isozaluzanin C (Dehydrozaluzanin c-derivative) is an anti-inflammatory agent that can be isolated from Saussurea lappa and has immunomodulatory effects. Isozaluzanin C improves tissue damage (lung, kidney, and liver) and excessive inflammation in mice induced by LPS (HY-D1056) or CRKP infection. Isozaluzanin C can be used in the study of bacterial infections and sepsi .
Shizukaol B is a lindenane-type dimeric sesquiterpene, used to be isolated from the whole plant of Chloranthus henryi. Shizukaol B has anti-inflammatory effect against lipopolysaccharide (LPS)-induced activation of BV2 microglial cells. Shizukaol B inhibits iNOS and COX-2, and suppresses NO production, TNF-α, and IL-1β expression .
Broussochalcone A is an antioxidant and an inhibitor of Xanthine Oxidase (IC50=2.21 μM), with free radical scavenging activity. Broussochalcone A inhibits iron-induced lipid peroxidation and nitric oxide synthesis in lipopolysaccharide (LPS) -activated macrophages. Broussochalcone A also induces Apoptosis of human renal carcinoma cells by increasing ROS levels and activating FOXO3 signaling pathways .
Fortunellin, is a flavonoid, that can be isolated from the fruits of Fortunella margarita (kumquat). Fortunellin exhibits little toxicity to mice and suppresses inflammation and ROS generation in H9C2 cells induced by LPS. Fortunellin protects against fructose-induced inflammation and oxidative stress by enhancing AMPK/Nrf2 pathway. Fortunellin can be used for diabetic cardiomyopathy research .
Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein .
Ginsenoside Rg2 (Standard) is the analytical standard of Ginsenoside Rg2. This product is intended for research and analytical applications. Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 inhibits VCAM-1 and ICAM-1 expressions stimulated with lipopolysaccharide (LPS). Ginsenoside Rg2 also reduces Aβ1-42 accumulation.
Hispolon, a polyphenol, can be isolated from Phellinus linteus. Hispolon possesses anticancer, antidiabetic, antioxidant, antiviral, hepatoprotective, anti-diabetic, and anti-inflammatory activities .
Coniferaldehyde (4-Hydroxy-3-methoxycinnamaldehyde) is an effective inducer of heme oxygenase-1 (HO-1). Coniferaldehyde inhibits LPS-induced apoptosis through the PKCα/β II/Nrf-2/HO-1 dependent pathway in RAW264.7 macrophage cells. Coniferaldehyde has antioxidant and anti-inflammatory activities .
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure .
Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibits the IKK Complex. Wedelolactone also inhibits 5-lipoxygenase (5-Lox) with an IC50 of 2.5 μM. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Wedelolactone can extract from Eclipta alba, and it can be used for the research of cancer .
Lewis X trisaccharide (Lewis X, Le x) is a potent TH2 regulator, antagonizes LPS-induced IL-12 immune expression. Lewis X trisaccharide is a human histo-blood group antigen, plays an key role in cell-cell adhesion, and servers as a tumor marker. Lewis X trisaccharide is highly expressed in the outer membrane of the parasite, can be used for the immunology research of schistosomiasis .
2'-Fucosyllactose (2'-FL) is an oligosaccharide that could be derived from human milk. 2'-Fucosyllactose regulates the expression of CD14, alleviates colitis and regulates the gut microbiome. 2'-Fucosyllactose stimulates T cells to increase IFN-γ production and decreases IL-6, IL-17, and TNF-α production of cytokines .
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone), a flavonoid compound, possesses potent anti-inflammatory effects in LPS-induced macrophage cell line mediated by inhibition of release of inflammatory mediators, NO, PGE2, and pro-inflammatory cytokines. 7,3',4'-Tri-O-methylluteolin significantly induces reduction in the mRNA expressions of inducible nitric oxide synthase and cyclooxygenase-2 .
Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway .
Santamarine (Santamarin), a sesquiterpene lactone, increases HO-1 expression through Nrf2 translocation and suppresses NO, PGE2, TNF-α, and IL-1β production through inhibition of NF-κB translocation in LPS-induced macrophages. Santamarine shows anti-photoaging properties via inhibition of MAPK/AP-1 and stimulation of TGF-β/Smad signaling in UVA-irradiated human dermal fibroblasts (HDFs). Antioxidant activities .
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta .
Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models , has selective inhibitory activity towards cyclooxygenase-2 (COX-2) .
Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways .
Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibits JNK and p38MAPK signals. Lucidone also has inhibitory activity against Dengue virus (DENV) (EC50=25 μM) .
Ethyl ferulate, a naturally lipophilic derivative of ferulic acid originally derived from Rhizoma Chuanxiong, induces heme oxygenase-1 (HO-1) and protects rat neurons against oxidative stress . Ethyl ferulate also protects neurons against amyloid β peptide (1-42)-induced oxidative stress and neurotoxicity .
Soyasapogenol B is a component of soy that has oral activity. Soyasapogenol B promotes autophagy and apoptosis. Soyasapogenol B has anti-inflammatory, antioxidant and antitumor activities .
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10 .
Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .
Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects .
4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR)TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model .
Narchinol B (Compound 4) is a sesquiter penoid
compound. Narchinol B has anti-inflammatory effects. Narchinol B works by
inhibiting proinflammatory mediators, including prostaglandin E2 (PGE2),
inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) proteins,
as well as proinflammatory cytokines, such as interleukin-1b, IL-6, and tumor
necrosis factor-α (TNF-α). Narchinol B significantly inhibits LPS-induced
overproduction of NO in BV2 cells (IC50=2.43 μM)
.
2,4,6-Trichlorol-3-methyl-5-methoxy-phenol 1-O-β-d-glucopyranosyl-(1 → 6)-β-d-glucopyranoside is a chlorophenyl glycoside found in the bulbs of Lilium brownie var. viridulum. 2,4,6-Trichlorol-3-methyl-5-methoxy-phenol 1-O-β-d-glucopyranosyl-(1 → 6)-β-d-glucopyranoside exhibits weak inhibition of NO production in LPS-stimulated RAW 264.7 cells .
1,3,5-Trihydroxy-4-prenylxanthone is a Na +/H + exchange system (Na+/H+ Exchanger (NHE)) inhibitor with a minimum inhibitory concentration of 10 μg/mL . 1,3,5-Trihydroxy-4-prenylxanthone is a phosphodiesterase type 5 (PDE5) (Phosphodiesterase (PDE)) inhibitor with an IC50 value of 3.0 μM . 1,3,5-Trihydroxy-4-prenylxanthone inhibits Lipopolysaccharide (LPS) (Lipopolysaccharides (HY-D1056))-induced NO production in RAW264.7 macrophages, and has anti-inflammatory activities .
Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties . Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways . Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM .
(3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid, a lanostane triterpenoids, exhibits obvious NO inhibitory activity on n LPS-induced BV-2 microglia cells with an IC50 of 9.55 uM. (3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid has anti-inflammatory activities .
Avicularin is an orally active flavonoid. Avicularin inhibits NF-κB (p65), COX-2 and PPAR-γ activities. Avicularin has anti-inflammatory, anti-infectious anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities .
The CXCR4 protein functions as a receptor for the CXC chemokine CXCL12/SDF-1, triggering an increase in intracellular calcium ions and activation of MAPK1/MAPK3. It is actively involved in AKT signaling, which is critical for regulating cell migration, especially in wound healing. CXCR4-VLPs Protein, Human (HEK293, His) is the recombinant human-derived CXCR4-VLPs protein, expressed by HEK293 , with C-10*His labeled tag. The total length of CXCR4-VLPs Protein, Human (HEK293, His) is 352 a.a., with molecular weight of 41.5 kDa.
Guaiacol-d3 is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Guaiacol has an anti-inflammatory activity[1].
Guaiacol-d7 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Guaiacol-d4 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Guaiacol- 13C6 is the 13C labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Guaiacol-d4-1 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Erdosteine- 13C4 is a 13C-labeled Erdosteine. Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation[1][2]. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects[3].
Beclometasone dipropionate-d10 is the deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
Beclometasone dipropionate-d6 is deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
Tolfenamic acid- 13C6 is the 13C6 labeled Tolfenamic acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
Tolfenamic acid-d4 is the deuterium labeled Tolfenamic Acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1[1][2].
Itaconate-alkyne (ITalk) is a specific bioorthogonal probe for quantitative and site-specific chemoproteomic profiling of Itaconation in living cells. Itaconate-alkyne, a functional analogue of Itaconate, exhibits comparable antiinflammatory effect with Itaconate and enables the labeling of bona fide targets of Itaconate . Itaconate-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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