Reactive Oxygen Species (ROS)

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.

2-Phospho-L-ascorbic acid trisodium acts as an antioxidant and a stimulator of hepatocyte growth factor (HGF) production.

Beta-Elemonic acid (3-Oxotirucallenoic Acid), a known triterpene isolated from Boswellia (Burseraceae), exhibits anti?inflammatory effects.

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.

Nexinhib20 is a selective inhibitor of the Rab27a-JFC1 interaction (IC50: 2.6 μM) and Rac-1-GTP signaling. This compound effectively inhibits neutrophil exocytosis, adhesion, and β2 integrin activation, demonstrating significant anti-inflammatory properties. Nexinhib20 is suitable for research applications focused on systemic inflammation and myocardial ischemia-reperfusion injury.

Lucigenin is a chemiluminescence probe primarily utilized for the detection of the endogenous superoxide anion radical (O2-). This compound exhibits high sensitivity and can also function as a chloride indicator, as its fluorescence is quenched in the presence of chloride ions. With excitation and emission wavelengths of 455 nm and 505 nm, respectively, Lucigenin serves as a valuable tool in studies involving reactive oxygen species and chloride ion interactions.

2′,7′-Dichlorofluorescein diacetate (DCFH2-DA) is a cell-permeable fluorescent probe utilized for the detection of reactive oxygen species (ROS). It becomes fluorescent upon cleavage by intracellular esterases and subsequent oxidation, allowing for the assessment of oxidative stress levels in biological systems. This reagent is essential for studies in toxicology and cellular signaling, enabling researchers to monitor and evaluate oxidative phenomena in various experimental contexts.

Berberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine (Natural Yellow 18) has antineoplastic properties. 

Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.

MitoSOX Red is a live cell fluorescent probe that specifically targets mitochondria and is cell membrane permeable. MitoSOX Red enters mitochondria and is oxidized by superoxide but not by other ROS or RNS generating systems. The oxidized MitoSOX Red then binds to nucleic acids in mitochondria/nucleus, producing strong red fluorescence. MitoSOX Red can be used as a fluorescent indicator to specifically detect superoxide. In addition, superoxide dismutase (SOD) can prevent the oxidation of MitoSOX Red. Excitation/emission wavelength: 510/580 nm.

Cylindrospermopsin, a cyanotoxin, is a polycyclic uracil derivative containing guanidine and sulfate groups, which can inhibit protein synthesis and covalently modify DNA or RNA. Cylindrospermopsin induces hepatocellular hypertrophy, renal cellular hypertrophy, intracellular reactive oxygen species (ROS), DNA strand breaks, mitochondrial hyperpolarisation, ultrastructural damage, and altered gene expression in liver, kidney, and intestinal cells. Cylindrospermopsin can be used in research including hepatocellular carcinoma and water quality testing.

Ciprofloxacin is a potent topoisomerase IV inhibitor that demonstrates significant antibacterial activity as a fluoroquinolone antibiotic. It induces both mitochondrial and nuclear DNA damage, leading to mitochondrial dysfunction and increased reactive oxygen species (ROS) production. Ciprofloxacin exhibits anti-proliferative properties and triggers apoptotic pathways, making it a valuable tool for research applications focused on bacterial infections, oxidative stress, and cancer biology.

10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis.

Lactobionic acid is a bionic acid that functions as a bacterial inhibitor, comprising gluconic acid and galactose. It exhibits potent antimicrobial and antioxidant properties, making it valuable in research related to food safety and microbiology. Lactobionic acid is effective against food-borne pathogens and has been shown to inhibit DNA repair, protein synthesis, and key metabolic pathways in methicillin-resistant Staphylococcus aureus (MRSA). Its applications extend to developing new functional products and enhancing food preservation.

HKOH-1 is a sensitive green fluorescent probe designed for the selective detection of hydroxyl radicals (·OH) in living cells, utilizing a maximum excitation wavelength of 500 nm and an emission wavelength of 520 nm. This reagent enables researchers to monitor oxidative stress and assess cellular responses to reactive oxygen species. Its application is critical in studies related to redox biology, neurodegenerative diseases, and cancer research.

5(6)-Carboxy-2',7'-dichlorofluorescein diacetate is a cell-permeant fluorescent indicator that targets reactive oxygen species (ROS) within cells. This reagent is particularly useful for monitoring ROS generation in human neuronal-glial (HNG) cells during primary co-culture experiments. Its ability to penetrate cellular membranes makes it a valuable tool for evaluating oxidative stress and related biological processes.

HKPerox-2 is a highly sensitive fluorescent probe specifically designed for the detection of hydrogen peroxide (H2O2) in live cells. It exhibits peak excitation and emission wavelengths at 520 nm and 543 nm, respectively, making it suitable for fluorescence microscopy applications. This reagent can be utilized to study oxidative stress and cellular signaling involving reactive oxygen species, enabling insights into various biological processes and disease mechanisms.

2',7'-Dichlorofluorescein is a potent fluorescent probe primarily used for the detection of oxidative stress by quantifying reactive oxygen species (ROS) levels. It exhibits excitation and emission maxima at 503 nm and 523 nm, respectively. This compound is essential for applications in cellular biology and biochemistry, enabling researchers to study oxidative damage and its effects on biological systems.

HKOH-1r is a highly sensitive green fluorescent probe designed for the selective detection of hydroxyl radicals (·OH) in living cells. It exhibits excitation and emission maxima at 500 nm and 520 nm, respectively, facilitating real-time visualization of oxidative stress. This reagent is applicable in various research settings, including studies focused on cellular redox status and oxidative damage pathways.

Diphenyl-1-pyrenylphosphine (DPPP) serves as a fluoregenic peroxide-reactive probe, facilitating the detection of reactive oxygen species. This compound exhibits a distinctive phototriggered aggregation-induced emission (AIE) and aggregation-induced quenching (ACQ) transition, showcasing significant alterations in its third-order nonlinear optical signals. DPPP is ideal for research applications involving oxidative stress and the study of ROS-related biological processes.

Solasonine is a naturally occurring steroidal glycoalkaloid isolated from *Solanum melongena* (eggplant), known for its anti-infective, anticancer, and neurogenesis-promoting properties. It acts as a ferroptosis inducer by disrupting the glutathione redox system through inhibition of glutathione peroxidase 4 (GPX4). By promoting ferroptotic cell death in hepatocellular carcinoma (HCC) cells, Solasonine serves as a valuable compound for investigating ferroptosis mechanisms and developing novel anticancer strategies.

Tin protoporphyrin IX dichloride (SnPPIX) is a potent inhibitor of heme oxygenase-1 (HO-1), an enzyme involved in cellular stress responses and tumor progression. SnPPIX has been shown to sensitize pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mouse models, enhancing therapeutic efficacy and supporting its potential use as a chemosensitizing agent in cancer treatment.

HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1) that induces apoptosis and suppresses cell migration by inhibiting the formation of invasive pseudopodia. It increases oxidative stress, activates the JNK/c-Jun pathway, and downregulates AKT and ERK signaling. HKB99 is a promising compound for the study of non-small cell lung cancer (NSCLC).

Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor that effectively blocks tyrosine autophosphorylation of ALK, mutant ALK, and EGFR, with IC50 values ranging from 5.38 to 16.74 nM. Additionally, it inhibits the transport activity of MATE1, MATE2K, P-gp, and BCRP. Iruplinalkib is under investigation for the treatment of non-small cell lung cancer (NSCLC).

Gondoic acid (cis-11-Eicosenoic acid) is a monounsaturated long-chain fatty acid found in various plant oils and nuts. It exhibits anti-inflammatory activity by reducing reactive oxygen species (ROS) production and inhibiting the PKCθ/ERK/STAT3 signaling pathway. Gondoic acid is also utilized as a raw material in medical applications and as a moisturizing agent in cosmetic formulations.

Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects.

ACA-28 (compound 2a) is a potent modulator of the ERK MAPK signaling pathway that exerts anticancer effects through a unique mechanism involving ERK hyperactivation. Rather than inhibiting ERK activity directly, ACA-28 induces sustained ERK activation, which paradoxically triggers apoptosis in cancer cells. It demonstrates selective cytotoxicity, inhibiting the growth of melanoma cells (SK-MEL-28) with an IC₅₀ of 5.3 μM, while showing lower toxicity toward normal human melanocytes (NHEM), with an IC₅₀ of 10.1 μM. ACA-28's ability to exploit ERK signaling dysregulation for selective induction of apoptosis makes it a promising candidate for further development in cancer therapy, particularly in ERK-dependent malignancies.

Cearoin is a bioactive compound that promotes both autophagy and apoptosis by inducing reactive oxygen species (ROS) production and activating the ERK signaling pathway. Through this dual mechanism, cearoin contributes to the regulation of cellular stress responses and programmed cell death. Its ability to modulate these processes makes it a valuable candidate for research in cancer biology and other diseases involving dysregulated autophagy or apoptosis.

Licochalcone D is a naturally occurring flavonoid primarily found in the root of *Glycyrrhiza uralensis* (Chinese licorice). It functions as a potent and orally active inhibitor of the NF-κB p65 subunit, a key regulator of inflammation and cancer-related signaling pathways. Licochalcone D exhibits broad pharmacological properties, including antioxidant, anti-inflammatory, and anticancer activities, making it a promising candidate for research in inflammation-related diseases and oncology.

PROTAC NCOA4 Degrader-1 (Compound V3) is a highly potent PROTAC targeting NCOA4, with a DC₅₀ of 3 nM in HeLa cells. It functions as a ferroptosis inhibitor by reducing NCOA4 levels and lowering intracellular ferrous iron (Fe²⁺) concentrations. PROTAC NCOA4 Degrader-1 has demonstrated protective effects in a CCl₄-induced acute liver injury model, making it a valuable tool for studying ferroptosis and liver disease therapeutics.

Fluoflavine is a selective inhibitor of NOX1 and reactive oxygen species (ROS) production. This compound effectively reduces ROS levels, NOX1-mediated signaling pathways, and prevents retinal ganglion cell death induced by oxygen-glucose deprivation. In preclinical studies, Fluoflavine has demonstrated the ability to inhibit NADPH oxidase activity and mitigate pathological retinal neovascularization in models of oxygen-induced retinopathy. It is a valuable tool for investigating retinal ischemia-reperfusion injury and proliferative retinopathy.