STING agonist-8 is a potent STING agonist with an EC50 of 27 nM in THP1-Dual KI-hSTING-R232 cells (WO2021239068A1, compound 5-AB)[1].
Anti-inflammatory agent 36 is an anti-inflammatory agent. Anti-inflammatory agent 36 inhibits LPS-induced macrophage activation[1].
Taurocholic acid sodium (Sodium taurocholate; N-Choloyltaurine sodium) has marked bioactive effects such as an inhibitory potential against hepatic artery ligation induced biliary damage by upregulation of VEGF-A expression. Immunoregulation effect[1].
Betamethasone-d5-1 is deuterium labeled Betamethasone. Betamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone accelerates fetal lung maturation and induces gene expression and apoptosis[1][2][3][4].
Cloperastine fendizoate inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM.
Ketoprofen (RP-19583) lysinate is a non-steroidal anti-inflammatory agent. Ketoprofen lysinate can inhibit the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity[1][2][3].
Coumarin is the primary bioactive ingredient in Radix Glehniae, named Beishashen in China, which possesses many pharmacological activities, including anticancer, anti-inflammation and antivirus activities.
Anti-MRSA agent 1 (Compound 13d) is a wonderful MRSA (MIC = 0.5 μg/mL) inhibitor. Anti-MRSA agent 1 (Compound 13d) could effectually relieve the development of MRSA resistance[1].
ATP dipotassium (Adenosine 5'-triphosphate dipotassium) is a central component of energy storage and metabolism in vivo, provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP dipotassium is an important endogenous signaling molecule in immunity and inflammation[1][2].
Furobufen, an anti-inflammatory agent, produces antiarthritic, antipyretic effects. Furobufen has an analgesic effect in inflamed tissue[1].
Demethoxycurcumin(Curcumin II) is a major active curcuminoid; possess anti-inflammatory properties; also exert cytotoxic effects in human cancer cells via induction of apoptosis.IC50 value: Target:in vitro: DMC significantly decreased NO secretion by 35-41% in our inflamed cell model. Decrease in NO production by DMC was concomitant with down-regulation of iNOS at mRNA and protein levels compared to proinflammatory cytokine cocktail and LPS-treated controls. Mechanism of action of DMC may be partly due to its potent inhibition of the iNOS pathway [1]. BDMCCN has the strongest inhibitory activity toward BACE-1 with 17 μM IC50, which was 20 and 13 times lower than those of CCN and DMCCN respectively [2]. Genes associated with DNA damage and repair, cell-cycle check point and apoptosis could be altered by DMC; in particular, 144 genes were found up-regulated and 179 genes down-regulated in NCI-H460 cells after exposure to DMC [3]. in vivo: At low doses, both the curcuminoid mixture and curcumin I did not affect brain stimulation reward, whereas, higher doses increased ICSS thresholds. Curcumin II and curcumin III did not affect brain stimulation reward at any doses. Subthreshold doses of the curcuminoid mixture and curcumin I inhibited the reward-facilitating effect of morphine.
Mycophenolic acid sodium is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 µM. Mycophenolic acid sodium demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid sodium is an immunosuppressive agent. Antiangiogenic and antitumor effects[1][2].
DHODH-IN-11 (Compound 14b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pKa of 5.03[1].
Artemitin is a flavonol found in Laggera pterodonta (DC.) Benth., with antioxidative, anti-inflammatory, and antiviral activity[1].
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta[1].Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models[2], has selective inhibitory activity towards cyclooxygenase-2 (COX-2)[1].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[3].
Lipopolysaccharides, Escherichiacoli (11C) consists of a hydrophobic lipid A, a core oligosaccharide (core OS), and a distal polysaccharide (O-PS). Lipopolysaccharides, Escherichiacoli (11C) can be used to induce inflammation[1].
L-Homocystine is the oxidized member of the L-homocysteine. Homocysteine is a pro-thrombotic factor, vasodilation impairing agent, pro-inflammatory factor and endoplasmatic reticulum-stress inducer used to study cardiovascular disease mechanisms.
GS143 is a selective IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 suppresses NF-κB activation and transcription of target genes and does not inhibit proteasome activity. GS143 has anti-asthma effect[1][2].
Kuwanon A is a flavone derivative isolated from the root barks of the mulberry tree (Morus alba L.); inhibits nitric oxide production with an IC50 of 10.5 μM.
Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent.
Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit CYP2C9 and CYP3A4.
Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain[1].
Procyanidin B1 is a polyphenolic flavonoid isolated from commonly eaten fruits, binds to TLR4/MD-2 complex, and has anti-inflammatory activity.
3-Hydroxy-2-(palmitoyloxy)propyl stearat is a non-volatile compound. 3-Hydroxy-2-(palmitoyloxy)propyl stearat can be isolated from less polar fractions of the brown macroalga Fucus virsoides J. Agardh. This part of the substance has a good ability to scavenge free radicals and has a protective effect on the oxidative stress induced by hydrogen peroxide in zebrafish embryos[1].
OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM.IC50 Value: 13 nM( Ki for hrCRTH2); 3 nM( Ki for Rat rCRTH2);13 nM(Ki for human native CRTH2)Target: D prostanoid receptor 2CRTH2 (chemoattractant receptor expressed on T-helper (Th) type 2 cells) is a G-protein-coupled receptor expressed by Th2 lymphocytes and eosinophils that mediates prostaglandin (PG)D(2)-driven chemotaxis[1]. CRTH2 mediates activation of Th2 cells, eosinophils and basophils in response to prostaglandin D(2). The CRTH2 antagonist OC000459 has been demonstrated to reduce airway inflammation and improve lung function in moderate persistent asthma[2].in vitro: OC000459 is an indole-acetic acid derivative that potently displaces [3H]PGD2from human recombinant DP2 (Ki = 0.013 μM), rat recombinant DP2 (Ki = 0.003 μM), and human native DP2 (Th2 cell membranes; Ki = 0.004 μM) but does not interfere with the ligand binding properties or functional activities of other prostanoid receptors (prostaglandin E1-4 receptors, D prostanoid receptor 1, thromboxane receptor, prostacyclin receptor, and prostaglandin F receptor). OC000459 inhibited chemotaxis (IC50 = 0.028 μM) of human Th2 lymphocytes and cytokine production (IC50 = 0.019 μM) by human Th2 lymphocytes. OC000459 competitively antagonized eosinophil shape change responses induced by PGD2 in both isolated human leukocytes (pKB = 7.9) and human whole blood (pKB = 7.5) but did not inhibit responses to eotaxin, 5-oxo-eicosatetraenoic acid, or complement component C5a. OC000459 also inhibited the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells. OC000459 had no significant inhibitory activity on a battery of 69 receptors and 19 enzymes including cyclooxygenase 1 (COX1) and COX2[3] .in vivo: OC000459 was found to be orally bioavailable in rats and effective in inhibiting blood eosinophilia induced by 13,14-dihydro-15-keto-PGD2 (DK-PGD2) in this species (ED50 = 0.04 mg/kg p.o.) and airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED50 = 0.01 mg/kg p.o.) [3].Clinical trial: N/A.
Dalutrafusp alfa (AGEN-1423; GS-1423) is a specific bifunctional antibody against CD73 and TGF-β, which is involved in the immunosuppressive pathway[1].
Tautomycetin is a potent and specifical PP1 inhibitor with the potential apoptosis-inducing activity. Tautomycetin inhibits purified PP1 and PP2A enzymes with IC50s of 1.6 nM and 62 nM, respectively. Tautomycetin is an antifungal antibiotic and has immunosuppressive effects in vivo. Tautomycetin can be used as a novel powerful tool to elucidate the physiological roles of PP1 in various biological events[1].
Escin IIa, isolated from horse chestnut, the seeds of Aesculus hippocastanum L., has positive effects on acute inflammation in animals. Escin IIa has gastroprotections on ethanol-induced gastric mucosal lesions in rats[1][2].
CJ-13,610, a nonredox-type 5-LO inhibitor, dose dependently suppresses 5-LO product formation in ionophore A23187-stimulated PMNL in the absence of exogenous AA with an IC50 of about 70 nM[1]. PMNL: polymorphonuclear leukocytes; AA: arachidonic acid
Arofylline is a PDE4 inhibitor as a potential treatment for asthma.