Reactive Oxygen Species (ROS) Activator

Iprodione is an orally active diformimide fungicide. Iprodione can specifically cause oxidative damage by producing free radicals (ROS). Iprodione is also an antiandrogen agent that delays adolescent development in rats and reduces sexual behavior and reproductive ability in rats.

Myrislignan is a PI3K/AKT/NF-κB inhibitor that can cross the blood-brain barrier. Myrislignan exerts anticancer activity by inducing apoptosis and ferroptosis. Myrislignan inhibits the replication and invasion of Toxoplasma gondii; it induces reactive oxygen species (ROS) imbalance, autophagy, and the death of Toxoplasma gondii tachyzoites. Myrislignan inhibits mitochondrial function and ERK1/2 phosphorylation to improve ovariectomy-induced osteoporosis. Myrislignan can be used in studies related to gastric cancer, glioblastoma, osteoporosis, and toxoplasmosis.

Macranthoside B is an apoptosis inducer with in vitro and in vivo anticancer activity. Macranthoside B induces autophagy and ferroptosis in cancer cells. Macranthoside B induces intracellular ROS accumulation, activates AMPK, inhibits mTOR and P70S6 kinase phosphorylation, and modulates Bcl-2/Bax expression. Macranthoside B activates caspase-3, caspase-9, and the intrinsic caspase cascade, induces PARP cleavage/degradation, and inhibits NRF2 signaling. Macranthoside B disrupts iron homeostasis via NCOA4-dependent ferritinophagy, up-regulates Lip-ROS, reduces mitochondrial membrane potential, and activates the JNK pathway. Macranthoside B can be used for the research of ovarian cancer, hepatoma, gastric carcinoma, breast carcinoma, colon carcinoma, glioma, melanoma, adenocarcinoma of the esophagogastric junction, and cervical cancer.

Psora-4 (5-(4-Phenylbutoxy) psoralen) is a selective K_v1.3 blocker (K_d = 3 nM). Psora-4 increases mitochondrial ROS production, activates stress response genes including daf-16 targets and heat shock proteins, reduces triglyceride accumulation, extends lifespan and healthspan in C. elegans, and increases resistance to Paraquat-induced oxidative stress. Psora-4 can be used for research on psoriasis and obesity.

Fomesafen is an orally active herbicide. Fomesafen inhibits protoporphyrinogen oxidase (PPO). Fomesafen induces Apoptosis and increases ROS. Fomesafen exhibits developmental toxicity, immunotoxicity, and neurotoxicity. It induces precancerous lesions in the liver and hepaturoporphyria in mice. Fomesafen is used to control broadleaf weeds in soybean fields, rubber plantations, and orchards.

1,3-Diphenylguanidine is a widely used accelerator in rubber vulcanization. 1,3-Diphenylguanidine increases ROS activity and decreases SOD and CAT activity. 1,3-Diphenylguanidine accelerates the vulcanization process. 1,3-Diphenylguanidine impairs the reproduction and growth of Moina macrocopa^{[1] [2] [3] .}

Flurochloridone (R-40244) is an orally active herbicide and an inducer of ER stress, apoptosis, and cytotoxicity. Flurochloridone upregulates GRP78 and activates the PERK-eIF2α-ATF4 UPR axis, ATF6, CHOP, Bax, and Bim. Flurochloridone decreases Akt, p-Akt, GSK3β, and p-GSK3β levels, and induces ROS, oxidative stress, γ-glutamyl cycle activation, and GSH accumulation. Flurochloridone inhibits mitochondrial respiration and ATP production while enhancing glycolysis and cell viability inhibition. Flurochloridone inhibits spermatogonial proliferation, spermatocyte meiosis, and sperm mitochondrial membrane potential, and induces Sertoli cell apoptosis and mitochondrial damage. Flurochloridone non-competitively binds phytoene desaturase, blocking phytoene desaturation and carotenoid synthesis, leading to leaf bleaching and phytotoxicity. Flurochloridone can be used for research on male reproductive toxicity, hepatotoxicity, and as a herbicide.

DIM-3,5-Cl2 is an inverse NR4A1/NR4A2 agonist with K_D values of 7.7 μM and 12.0 μM for NR4A1 and NR4A2, respectively. DIM-3,5-Cl2 acts as an inverse agonist to downregulate pro-oncogenic and proendometriotic gene products, and as an agonist to enhance NR4A1/2/Sp1/Sp4-mediated CD71 transactivation. DIM-3,5-Cl2 induces ferroptosis via ROS formation, lipoperoxidation, MDA production, and reduced GPX4, SLC7A11 expression. DIM-3,5-Cl2 induces apoptosis via PARP and caspase-3 cleavage, reduced BCL-2 expression, and inhibits cancer cell viability. DIM-3,5-Cl2 can be used for the research of triple negative breast cancer, endometriosis, and colorectal cancer.

(E)-2-Octenal is an Antifungal agent. (E)-2-Octenal disrupts cell membrane integrity and causes ROS accumulation. (E)-2-Octenal decreases the activities of phosphofructokinase and pyruvate kinase. (E)-2-Octenal inhibits Neofusicoccum parvum growth by disrupting mitochondrial energy metabolism. (E)-2-Octenal suppresses the growth of a Prochloraz (HY-B0845)-resistant Penicillium italicum strain. (E)-2-octenal exerts a broad-spectrum and potent inhibitory effect on various fungi, including Sclerotium rolfsii, Metarhizium anisopliae sensu lato, and Aspergillus flavus, etc. (E)-2-Octenal can be used for the research of citrus blue mold and mango stem-end rot.

Actein, a triterpene glycoside, shows an inhibitory effect on cancer cells, which is isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in bladder cancer. Actein has little toxicity in vivo.

Physalin B is an orally active anti-inflammatory and anticancer agent. Physalin B can be isolated from Physalis alkekengi L. var. Franchetii. Physalin B inhibits the activation of the NF-κB, NLRP3 inflammasome, STAT3, PI3K/Akt and Hedgehog signaling pathways, regulates the phosphorylation levels of GSK-3β, p38 MAPK, ERK1/2 and JNK, and promotes the nuclear translocation of NRF2. Physalin B reduces the levels of pro-inflammatory cytokines and factors, induces mitochondrial reactive oxygen species (mito-ROS) production, Apoptosis, G2/M cell cycle arrest and incomplete Autophagy, alters cytoskeleton structure and alleviates oxidative stress. Physalin B reduces cancer cell viability, ameliorates liver and lung tissue damage and alleviates liver fibrosis. Physalin B can be used in research related to ulcerative colitis, breast cancer, acute lung injury, colon cancer, non-alcoholic steatohepatitis, liver fibrosis, lung cancer, pancreatic cancer, lymphoma, ovarian cancer, sarcoma and leukemia.

Cereulide is an orally active, blood-brain barrier-permeable emetic toxin. Cereulide acts as a potassium ionophore that inserts into membranes, forms complexes with K⁺, and transports K⁺ from the cytoplasm into the mitochondrial matrix. Cereulide disrupts the electrochemical gradient of the inner mitochondrial membrane, leading to mitochondrial swelling and dysfunction, uncoupling of oxidative phosphorylation, inhibition of ATP synthesis, ROS accumulation, and ultimately triggering apoptosis and autophagy. Cereulide exhibits multi-organ toxicity and can be used for research on emetic food poisoning.

Massoia lactone ((±)-Massoia lactone) is a natural lactone-based biosurfactant with antifungal (fungal), antibiofilm, and cytotoxic activities. Massoia lactone inhibits fungal hyphal growth and spore germination, and induces fungal cell necrosis by forming membrane pores, reducing ergosterol, elevating ROS, and causing leakage of intracellular components. Massoia lactone inhibits the viability and proliferation of tumor cells. Massoia lactone degrades the extracellular polymeric substances of polymicrobial biofilms, penetrates the biofilm matrix, inhibits the growth of planktonic oral bacteria (bacterial), and reduces surface tension through its amphiphilic properties. Massoia lactone is a low-toxicity, biodegradable food additive with a coconut cream aroma, which can be used for flavor improvement and also serves as a quality control marker for Cs-4 mycelium. Massoia lactone can be used for research on Fusarium head blight, malignant tumors, and oral polymicrobial biofilm-associated dental diseases.

SKLB-D18 is an orally active ERK1/2/ERK5 inhibitor, with an IC₅₀ of 38.69 nM and a K_d of 126.9 nM against human ERK1, an IC₅₀ of 40.12 nM and a K_d of 209.8 nM against ERK2, and an IC₅₀ of 59.72 nM and a K_d of 468.2 nM against ERK5. SKLB-D18 inhibits cancer cell proliferation, induces G0/G1 cell cycle arrest and apoptosis. SKLB-D18 reduces the levels of p-ERK5, p-RSKp90, p-c-Myc and c-Myc, and upregulates the level of p-ERK1/2, thereby inhibiting the ERK1/2/5 pathway in cells. SKLB-D18 increases LC3B-II accumulation, and decreases the levels of p62, p-mTOR and p-p70S6K. SKLB-D18 elevates the levels of ROS, lipid peroxidation and free ferrous ions, reduces the levels of NCOA4 and GPX4, and induces ferritin autophagy-dependent ferroptosis in cancer cells. SKLB-D18 exhibits antitumor activity in a triple-negative breast cancer xenograft mouse model. SKLB-D18 can be used in research related to triple-negative breast cancer.

GPX4-IN-19 is an effective GPX4 inhibitor (IC₅₀ = 0.311 μM), covalently binds to the Sec 46 site of GPX4. GPX4-IN-19 shows strong anti-proliferative activity with high ferroptosis selectivity. GPX4-IN-19 causes intracellular Fe²⁺ accumulation, leading to increased levels of lipid peroxides (LPOs) and reactive oxygen species (ROS), which induces ferroptosis and subsequently results in DNA damage. GPX4-IN-19 can be used for the study of Triple-Negative Breast Cancer (TNBC).

Fenobucarb is a carbamate insecticide. Fenobucarb induces zebrafish developmental neurotoxicity through pathways involved in inflammation, oxidative stress, degeneration and apoptosis. Fenobucarb is a possible risk factor to cardiovascular and cerebrovascular systems in animals.

Trabectedin D₃ (Ecteinascidin 743 D₃) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment.

Cearoin increases autophagy and apoptosis through the production of ROS and the activation of ERK.

Tetrahydroxyquinone (Tetrahydroxy-1,4-benzoquinone), a primitive anticataract agent, is a redox active benzoquinone. Tetrahydroxyquinone can take part in a redox cycle with semiquinone radicals, leading to the formation of reactive oxygen species (ROS).

Cereulide-¹³C₆ is a deuterated form of Cereulide. Cereulide is an orally active, blood-brain barrier-permeable emetic toxin. Cereulide acts as a potassium ionophore that inserts into membranes, forms complexes with K⁺, and transports K⁺ from the cytoplasm into the mitochondrial matrix. Cereulide disrupts the electrochemical gradient of the inner mitochondrial membrane, leading to mitochondrial swelling and dysfunction, uncoupling of oxidative phosphorylation, inhibition of ATP synthesis, ROS accumulation, and ultimately triggering apoptosis and autophagy. Cereulide exhibits multi-organ toxicity and can be used for research on emetic food poisoning.