TLR7 agonist 4 (Compound 1.2) is a TLR7 agonist with an EC50 of 4.3 nM[1].
cGAMP(Cyclic GMP-AMP) is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA; STING ligand.Target:in vitro: cGAMP induced IFNβ RNA robustly even at concentrations as low as 10 nM. cGAMP was much more potent than c-di-GMP in inducing IFNβ based on ELISA assays. cGAMP was also more potent than c-di-GMP and c-di-AMP in activating IRF3. cGAMP binds to and activates STING to trigger the downstream signaling cascades [1]. On stimulation with cGAMP, fibroblasts from the patients showed increased transcription of IFNB1 but not of the genes encoding interleukin-1 (IL1), interleukin-6 (IL6), or tumor necrosis factor (TNF) [3]. cGAMP activates the endoplasmic reticulum (ER)-resident receptor STING, thereby inducing an antiviral state and the secretion of type I IFNs [4].in vivo: cGAMP can enhance the adaptive immune response to the model antigen ovalbumin in mice. cGAMP promotes antigen specific IgG and a balanced Th1/Th2 lymphocyte response in immunized mice [2].
Danicopan, a selective and orally active small-molecule factor D inhibitor, inhibits alternative pathway of complement (APC) activity. Danicopan has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS)[1].
Alistin (Carcinine; β-Alanylhistamine) is a selective histamine H3 antagonist with antioxidant activity and neuroprotective effects on the retina of oxidatively stressed mice[1][2].
PDM2 is a selective, high-affinity aryl hydrocarbon receptor (AhR) antagonist with an Ki of 1.2±0.4 nM.
Ezabenlimab (BI-754091) is an anti-PD-1 mAb with binding constant Kd value of 6 nM (CHO cells). Ezabenlimab blocks the interaction of PD-1 with PD-L1 and PD-L2. Ezabenlimab increases interferon-γ secretion in T cells, and inhibits tumor growth in vivo[1].
Friluglanstat is a prostaglandin E synthase (mPGES-1) inhibitor, with anti-inflammatory activity[1].
Inolimomab is an anti-interleukin-2 receptor (IL-2R) α chain monoclonal antibody. Inolimomab improves the survival rate of patients in the early research of treating acute graft-versus-host disease (aGVHD)[1][2].
Rilonacept (Arcalyst), a dimeric fusion protein, is a interleukin 1 inhibitor. Rilonacept consists of the ligand-binding domains of the extracellular portions of the IL-1R components linked to the Fc portion of human IgG1. Rilonacept can be used for the research of cryopyrin-associated periodic syndromes[1].
Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with high affinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases[1].
Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.
Nivolumab (anti-PD-1) is a programmed death receptor-1 (PD-1) blocking human IgG4 antibody to treat advanced (metastatic) non-small cell lung cancer[1].
γ-Tocopherol-d4 (D-γ-Tocopherol-d4) is the deuterium labeled γ-Tocopherol. γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity[1][2].
Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.
Triptoquinone A, an interleukin 1 inhibitor, inhibits endomycin (LPS) or interleukin (IL-1β)-promoted induction of nitric oxide synthase (NOS) in vascular smooth muscle, thereby inhibiting Arg-induced vascular relaxation[1].
Rubranol is an inhibitor of NO Synthase. Rubranol inhibits LPS-induced NO production in activated macrophages with 74% inhibition[1].
Buddlejasaponin IV (BS‐IV) exerts anti-inflammatory and cytotoxic effects against cancer cells[1].
Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB)[1][2].
PROTAC IRAK4 degrader-8 (compound 2) is a PROTAC targeting to IRAK4 (IC50=15.5 nM)[1].
C5aR-IN-1 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-1 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 47)[1].
Sinapyl alcohol is an orally active anti-inflammatory and antinociceptive agent. Sinapyl alcohol reduces the expression level of inducible NO synthase and COX-2[1].
Limaprost(OP1206) is a PGE1 analog and potent platelet adhesion inhibitor.Target: OthersLimaprost, an alprostadil (prostaglandin E1) analogue, is a vasodilator that increases blood flow and inhibits platelet aggregation. Limaprost is a n analog of PGE1 with structural modifications intended to give a prolonged half-life and greater potency. It is orally active in both guinea pigs and rats at doses of 100 mg/kg as an inhibitor of ADP and collagen induced platelet aggregation. It is 10-1,000 times more potent than PGE1 as a platelet adhesive inhibitor, measured in vitro. Intra-coronary injection (100 ng/kg) or intravenous injection (3 mg/kg) in anesthetized dogs causes vasodilation and increased coronary blood flow by 60-80%. Significant hypotensive effects were seen at 100 and 300 mg/kg orally in rats [1].
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[1].
Troxerutin, also known as vitamin P4, is a tri-hydroxyethylated derivative of natural bioflavonoid rutins which can inhibit the production of reactive oxygen species (ROS) and depress ER stress-mediated NOD activation.
Danburstotug (IMC-001) is an IgG1-lambda anti-CD274 (PDL1, B7 homologue 1, B7H1) humanized monoclonal antibody. Danburstotug also is immunostimulant and antineoplastic[1].
COX-2-IN-36 (compound 1) is a very potent and specific COX-2 inhibitor, with an IC50 of 0.4 μM[1][2].
ARL-17477 is a dual inhibitor of NOS1and the autophagy-lysosomal system with anticancer activity and can inhibit tumor growth in KRAS-mutated cancers[1].
PTUPB is a novel dual acting COX-2/sEH inhibitor with IC50 of 1.26 uM/0.9 nM,does not inhibits COX-1 (IC50>100 uM); reduces kidney injury parameters, decreases inflammatory and oxidative stress markers in ZDF rats; exhibits more effective than the same dose of either COX-2 inhibitor (celecoxib) or sEH inhibitor (t-AUCB) alone, shows in vivo antiallodynic activity in vivo; also suppresses glioblastoma growth by targeting EGFR and hyaluronan mediated motility receptor, potentiates the antitumor efficacy of cisplatin.
IL-17A inhibitor 1 (example 24) is a IL-17A inhibitor, with IC50 values of <9.45 nM and 9.3 nM in alphalisa assay and HT-29 cells[1].
Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38[1].