Orniplabin (SMTP-7) is a low-molecular-weight compound that enhances plasminogen–fibrin binding, urokinase-catalyzed activation of plasminogen, and urokinase and plasminogen-mediated fibrin degradation. Orniplabin shows potential thrombolytic and anti-inflammatory effects. Orniplabin inhibits ROS[1][2].
AChE/BChE/BACE-1-IN-2 (Compound 4o) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.069, 0.127 and 0.097 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-2 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-2 has remarkable antioxidant potential[1].
ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.058, 0.082 and 0.115 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-1 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-1 has remarkable antioxidant potential[1].
APG-2449 is an orally active ALK/ROS1/FAK inhibitor. APG-2449 shows antitumor activity in mouse models of non-small cell lung cancer (NSCLC)[1].
Antimicrobial agent-2 (compound V-a) is a broad-spectrum antimicrobial agent, possessing inhibitory activity against various Gram-positive and -negative bacteria. Antimicrobial agent-2 has excellent inhibitory effect on Methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 1 μg/mL. Antimicrobial agent-2 can effectively damage the membrane and lead to the leakage of protein, also can induce the generation of ROS. Antimicrobial agent-2 exhibits low toxicity, no obvious resistance and good bioavailability[1].
GGTI-2133 is a direct and selective inhibitor of geran ylgeranyltransferase (GGTase). GGTI-2133 has the potential for eosinophilic airway inflammation such as asthma research[1].
Bixin (BX), isolated from the seeds of Bixa orellana, is a carotenoid, possessing anti-inflammatory, anti-tumor and anti-oxidant activities. Bixin treatment ameliorated cardiac dysfunction through inhibiting fibrosis, inflammation and reactive oxygen species (ROS) generation[1].
β-Carotene-d10 (Provitamin A-d1) is the deuterium labeled β-Carotene. β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities[1][2][3][4][5].
Antiproliferative against-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative against-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative against-7 can increase ROS production and induce apoptosis[1].
Neohesperidin dihydrochalcone is a synthetic glycoside chalcone, is added to various foods and beverages as a low caloric artificial sweetener.
Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins inhibitor with Ki values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis[1] and autophagy[2]. Apogossypolone also has antifungal activity[3].
Mammea A/BA has potent activity against Trypanosoma cruzi (T. cruzi). Mammea A/BA induces mitochondrial dysfunction, ROS production and DNA fragmentation, and increases number of acidic vacuoles. Mammea A/BA can induce apoptosis, autophagy and necrosis. Mammea A/BA can be used for researching chagas disease[1].
Pinealon is a 3-amino acid peptide and shows neuroprotective properties. Pinealon prevents reactive oxygenspecies (ROS) accumulation and supressesthe activation of ERK 1/2. Pinealon has the ability to stimulate the functional activity of the main cellular elements of brain tissue, reduce the level of spontaneous cell death. Pinealon protects the rat offspring from prenatal hyperhomocysteinemia[1][2][3].
Entrectinib is a potent and orally available Trk, ROS1, and ALK inhibitor; inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively.
Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model[1].
Taletrectinib (DS-6051b) is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants[1][2].
Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer[1][2].
Phyltetralin (Compound 10) is a natural product than can be isolated from the hexane-ethyl acetate extract of Phyllanthus amarus leaves. Phyltetralin possesses immunosuppressive effects on different lineages of innate immune system[1][2].
Methyl 12-methyltridecanoate ((R)-betaxolol hydrochloride) is a biosurfactant extracted from Brevibacterium casei LS14.Methyl 12-methyltridecanoate provides a novel approach for functionalizing the silver nanoparticles higher biocompatibility in vivo environmental[1].
DPP-4 inhibitor 3 (Compound 5a) is a potent dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 0.75 nM. DPP-4 inhibitor 3 shows excellent antioxidant and insulinotropic activity[1].
Picroside II, an iridoid compound extracted from Picrorhiza, exhibits anti-inflammatory and anti-apoptotic activities. picroside II alleviates the inflammatory response in sepsis and enhances immune function by inhibiting the activation of NLRP3 inflammasome and NF-κB pathways[1]. Picroside II is an antioxidant, exhibits a significant neuroprotective effect through reducing ROS production and protects the blood-brain barrier (BBB) after cerebral ischemia-reperfusion (CI/R) injury[2].
Capillarisin, as a constituent from Artemisiae Capillaris herba, is found to exert anti-inflammatory and antioxidant properties. Capillarisin can be used for the research of asthma-mediated complications and can be a potential neuroprotectant against bupivacaine-induced neurotoxicity[1][2][3].
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively[1].
Lorlatinib-d3 is the deuterium labeled Lorlatinib. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALKL1196M
Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A[1]. Lactacystin inhibits cell growth and induces neurite outgrowth[2].
Anti-inflammatory agent 21 (compound 9o) is an orally active and low cytotoxic anti-inflammatory agent, with an IC50 value of 0.76 μM for NO. Anti-inflammatory agent 21 acts via accumulation ROS and blocks the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 21 can ameliorate cartilage destruction and inflammatory cell infiltration in arthritis rats model[1].
GGTI-2147 is a potent GGTase I inhibitor. GGTI-2147 blocks geranyl-geranylation of Rap1A and reduces the activity of Rac1 (one of substrates for GGTI) and ameliorates the OGD/R-induced neuronal apoptosis.GGTI-2147 can be used for neurodevelopmental disorders research, such as autism, depression, and schizophrenia[1].
Huangjiangsu A, pseudoprotodioscin, methyl protobioside, protodioscin, and protodeltonin, isolated from D. villosa. Huangjiangsu A has hepatoprotective potential against H2O2-induced cytotoxicity and ROS generation and could be promising as potential therapeutic agents for liver diseases[1].
DMNQ is a redox cycling agent that generates both superoxide and hydrogen peroxide intracellularly in a concentration dependent manner. DMNQ increases ROS generation[1].