Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
Fosifidancitinib is a potent and selective inhibitor of JAK kinases 1/3. Fociatinib is used in studies of allergies, asthma and autoimmune diseases[1].
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[1][2].
Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1].
Angelicain (Norcimifugin) is a constituent of Cimicifuga foetida with anti-inflammatory activity[1].
Nargenicin A1 is an antibiotic agent against various Gram-positive bacteria. Nargenicin A1 shows anti-inflammatory activity. Nargenicin A1 protects HINAE cells against Tacrolimus (HY-13756)-induced DNA damage and apoptosis. Nargenicin A1 can also be used for the research of acute myeloid leukemia[1].
Piketoprofen is a non-steroidal anti-inflammatory reagent that can be used as a cream preparation for the study of soft tissue rheumatism[1].
Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2)[1][2][3].
Trans-Trimethoxyresveratrol is a derivative of Resveratrol (RSV),and it may be a more potent anti-inflammatory, antiangiogenic and vascular-disrupting agent when compared with resveratrol.In vitro: The in vitro study of resveratrol and trans-Trimethoxyresveratrol showed rather weak cytotoxic effects on three cancer cell lines (HepG2, MCF-7, and MDA-MB-231), which contradicted a previous study reporting that resveratrol inhibited MCF-7 cells with an IC50 of about 10?μM. This discrepancy might be explained by the fact that the measurements were made 24?h after drug treatment, whereas the measurements of the previous study were taken 6 days after. The fact that the cytotoxic effect of trans-Trimethoxyresveratrol was lower than that of resveratrol is surprising, because in many studies, trans-Trimethoxyresveratrol is the most active analogue of resveratrol , although resveratrol shows much stronger antioxidant effects than that of trans-Trimethoxyresveratrol.[1]In vivo: Zebrafish embryos offer great advantage over their adults as well as other in vivo models because of the external development and optical transparency during their first few days, making them invaluable in the inspection of developmental processes. These unique advantages can even be made more useful when specific cell types are labeled with fluorescent probes. Zebrafish embryo in vivo, suggests that trans-Trimethoxyresveratrol has both more potent antiangiogenic activity and more importantly, stronger specific cytotoxic effects on endothelial cells than does resveratrol.[1]
L-Leucyl-L-Leucine methyl ester (LLOMe) hydrobromide, a dipeptide condensation product of L-leucine methyl ester generated by human monocytes or polymorphonuclear leukocytes, selectively eliminates lymphocytes with cytotoxic potential. L-Leucyl-L-Leucine methyl ester hydrobromide also can induce endolysosomal pathway stress[1][2][3].
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.
Suxibuzone is a drug used for joint and muscular pain, is a prodrug of the non steroidal anti inflammatory drug Phenylbutazone.
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].
GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC50 value of 4 nM for HEK-293 cell.
JAK3-IN-9 is an orally active JAK3 inhibitor with IC50 value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research[1].
trans-Chalcone, isolated from Aronia melanocarpa skin, is a biphenolic core structure of flavonoids precursor. trans-Chalcone is a potent fatty acid synthase (FAS) and α-amylase inhibitor. trans-Chalcone causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7. trans-Chalcone has antifungal and anticancer activity[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.
Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory[1][2][3].
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].
Oxyphyllenone A is an inhibitor of NO Synthase. Oxyphyllenone A inhibits the NO production in lipopolysaccharide-activated macrophages with an IC50 of 28 μM[1].
Artemitin is a flavonol found in Laggera pterodonta (DC.) Benth., with antioxidative, anti-inflammatory, and antiviral activity[1].