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Acetylcysteine is a pharmaceutical drug and nutritional supplement used primarily as a mucolytic agent and in the management of paracetamol (acetaminophen) overdose. Oral acetylcysteine is also used for the prevention of radiocontrast-induced nephropathy (a form of acute renal failure).
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- R Kasi, .et al. , Clinical Cancer Drugs, 2020, 2019, 7(1): 44 - 56
- Allopurinol is a purine analog; it is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase.
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xanthine oxidase inhibitor
Allopurinol is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase. -
Berberine hydrochloride was novelly found that it has various beneficial effects on the cardiovascular system and significant anti-inflammatory activities. Berberine can effectively reduce intracellular superoxide levels in LPS-stimulated macrophages. Such a restoration of cellular redox by berberine is mediated by its selective inhibition of gp91phox expression and enhancement of SOD activity.
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Dihydropyrimidinase Inhibitor
Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects. -
xanthine oxidase inhibitor
Febuxostat is a non-purine inhibitor of xanthine oxidase (Ki = 1.2 nM). - TPEN is a heavy metal chelator. Reacts with both Zn-proteome and Zn-metallothionein (MT) in LLC-PK1 cells; acts as an intracellular chelator of proteomic Zn2+.
- Trabectedin (Ecteinascidin-743 or ET-743) is a novel antitumour agent of marine origin with potent antitumour activity both in vitro and in vivo.
- Benzenepentacarboxylic acid (BA), a novel fluorescent probes to detect and scavenge HO-.
- 6-Benzylaminopurine is a first-generation synthetic cytokinin which could regulate the activities of the antioxidant defense system of plants.Its treatment elicits plant growth and development.
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HO-1 inhibitor
Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is a competitive heme oxygenase-1 (HO-1) inhibitor, markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2.- Beixian Zhou, .et al. , MedComm, 2024, Apr 12;5(4):e531 PMID: 38617435
- Sulcotrione is a β-triketone herbicide which can inhibit hydroxyphenylpyruvate dioxygenase (HPPD).
- Ecabet sodium is a widely employed mucoprotective agent for the treatment of gastric ulcers.
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elastogenesis inhibitor
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. -
TRK, ROS1, ALK inhibitor
Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity.- Angelina T Regua, .et al. , Cancer Lett, 2024, Jun 7:597:217023 PMID: 38852701
- MCLA is a Cypridina luciferin analog that is used to detect superoxide generated by activated leukocytes and macrophages.
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Antioxidants
Glutathione oxidized, or GSSG, results from glutathione undergoing oxidation. It plays a crucial role in neutralizing reactive oxygen species, a process that concurrently generates GSSG. This oxidized form of glutathione is pivotal in studies concerning sickle cells and erythrocytes, where it's utilized for research purposes.
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Antioxidant
Ethoxyquin is an antioxidant that is widely used in animal feed to protect against lipid peroxidation and fat rancidity in chicken, salmon, and beef. - Mitoquinone is a mitochondria-targeted antioxidant designed to accumulate within mitochondria in vivo in order to protect against oxidative damage.
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antioxidant
α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. -
Topoisomerase IV inhibitor
Ciprofloxacin Hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, interfering with the bacterial DNA gyrase, inhibiting the DNA synthesis, and preventing bacterial cell growth.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
- Norgestrel is a synthetic analog of progesterone, a compound commonly found in oral contraceptive pill, and a powerful neuroprotective antioxidant, preventing light-induced ROS in photoreceptor cells, and cell death.
- Temoporfin(KW 2345) used in photodynamic therapy for the treatment of squamous cell carcinoma of the head and neck. Target: Others Temoporfin used in photodynamic therapy for the treatment of squamous cell carcinoma of the head and neck. Patients can remain photosensitive for several weeks after treatment.
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thromboxane A2 (TXA2) receptor (TP receptor) antagonist
Seratrodast is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma. - Pyropheophorbide-a (Ppa) is a promising photosensitizer for tumor photodynamic therapy (PDT).
- Purpurin 18, a derivative of chlorophyll, is an interesting dihydroporphyrin for generating photosensitizers.
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ERRγ agonist
GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
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RUNX2-DNA binding inhibitor
CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM. CADD522 exhibits antitumor activity.- Jiten R Sharma, .et al. , Life Sci, 2023, Apr 1;318:121480 PMID: 36775116
- N-Acetylcysteine amide is a cell membranes and blood brain barrier permeant thiol antioxidant and neuroprotective agent, reduces ROS production.
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ROS1/TRK inhibitor
Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM), TRK (0.83/0.05/0.1 nM=TRKA/B/C) inhibitor. - Mito-TEMPO is a mitochondria-targeted superoxide dismutase mimetic with superoxide and alkyl radical scavenging properties.
- Panpan Tai, .et al. , J Transl Med, 2023, Nov 17;21(1):823 PMID: 37978379
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Wnt/β-catenin activator
Methyl vanillate, one of the ingredients in Hovenia dulcis Thunb, is a Wnt/β-catenin pathway activator. A benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite. - L-Theanine (L-Glutamic Acid ??-ethyl amide??is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective and anti-oxidative activities.
- Succinobucol is a phenolic antioxidant with anti-inflammatory and antiplatelet effects.
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haemoglobin allosteric modifier
Efaproxiral sodium is a synthetic allosteric modifier of haemoglobin (Hb), decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy. -
KGDHC inhibitor
Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. - Mitoquinone mesylate is a TPP-based, mitochondrially targeted antioxidant in order to protect against oxidative damage.
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tubulin polymerisation inhibitor
Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulin polymerisation inhibitor with IC50 of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. -
ROS1/NTRK inhibitor
Taletrectinib (DS-6051b) is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. - Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities.
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antioxidant
2-Phospho-L-ascorbic acid trisodium acts as an antioxidant and a stimulator of hepatocyte growth factor (HGF) production. -
COX activator
Beta-Elemonic acid (3-Oxotirucallenoic Acid), a known triterpene isolated from Boswellia (Burseraceae), exhibits anti?inflammatory effects. -
nervoussystem toxicant
Emamectin Benzoate (MK-244) is an orally active nervoussystem toxicant by binding g-aminobutyric (GABA) receptor in insects. - Norbergenin, also known as Demethylbergenin, is the O-demethyl derivative of bergenin, the main component of Mallotus japonicus.It shows moderate antioxidant activity with IC(50)= 13 μM in DPPH radical scavenging and 32 μM in superoxide anion scavenging.