iNOS Activator

Agatolimod ((ODN 2006; PF-3512676; CpG 7909)) is a TLR9 agonist and immunomodulator with an EC₅₀ of 180 nM against human TLR9. Agatolimod activates and upregulates the expression of both TLR9 and TLR6, and mediates downstream signaling pathways via IRAK4, IRF5, IRF7. Agatolimod induces Th1-type innate and adaptive immune responses, activates various immune cells and promotes antigen presentation, regulates antibody levels and immune cell infiltration, upregulates the secretion of multiple cytokines, induces apoptosis and cell cycle arrest, enhances cytotoxicity, and clears intracellular Salmonella. Agatolimod is applicable to research on COVID-19, breast cancer, lung adenocarcinoma, HPV-related tumors, melanoma, and salmonellosis.

7,8-Dihydroneopterin, an inflammation marker, induces cellular apoptosis in astrocytes and neurons via enhancement of nitric oxide synthase (iNOS) expression. 7,8-Dihydroneopterin can be used in the research of neurodegenerative diseases.

Quinocetone is an orally active animal feed additive used to increase the meat production of livestock and poultry. Quinocetone exhibits antibacterial activity against a variety of pathogenic microorganisms. Quinocetone exhibits tissue-specific (liver, lymphocyte) toxicity. Quinocetone induces autophagy in cells through the ATF6/DAPK1 pathway. Quinocetone activates the NF-κB and iNOS pathways, leading to cell apoptosis, hepatocyte vacuolar degeneration and fibrosis. Quinocetone can inhibit Nrf2/HO-1 and induce the generation of reactive oxygen species (ROS), leading to oxidative stress and DNA damage.

Benzanthrone is an immunotoxic, pro-inflammatory Photosensitizer. Benzanthrone upregulates iNOS, COX-2 and inflammatory cytokines; activates ERK1/2, p38, JNK, AP-1 and NF-κB; inhibits Nrf2; and induces oxidative stress and DNA damage. Upon radiation exposure, Benzanthrone generates singlet oxygen and superoxide anion radicals, induces photohemolysis and lipid peroxidation, and alters the levels of skin xenobiotic enzymes. Benzanthrone exhibits differential genotoxicity in different cell lines. Benzanthrone possesses skin tumor-initiating and promoting activities. Benzanthrone can be used in skin tumor-related studies.

Banoxantrone (AQ4N), as a prototype hypoxia selective cytotoxin, can be reduced to AQ4, a potent topoisomerase II inhibitor. Banoxantrone selectively kills hypoxic cells via an iNOS-dependent mechanism. Banoxantrone shows a potent cytotoxicity and hypoxia-selective effect enhanced by radiation.

Anabsinthin is a dimeric sesquiterpene lactone. Anabsinthin can be found in Artemisia absinthium L. (wormwood). Anabsinthin modulates intracellular calcium levels, mediates anti-inflammatory and antioxidant effects. Anabsinthin inhibits Phorbol 12-myristate 13-acetate (HY-18739)-induced superoxide anion production, increased iNOS and MUC5AC protein expression, and IL-1β transcription upregulation. Anabsinthin can be used for the research of citrus canker.

PSB 0474 (3-phenacyl-UDP) is a UDP (HY-113359) analog and selective P2Y₆ receptor agonist, with an EC₅₀ value of 70 nM for the hP2Y₆ receptor. PSB 0474 activates Phospholipase C-coupled receptors to increase intracellular inositol phosphate levels. PSB 0474 enhances NO release by upregulating inducible iNOS and induces Apoptosis. PSB 0474 increases micturition frequency in urine of anesthetized rats, without altering bladder contraction amplitude/duration or causing urothelial damage. PSB 0474 can be used in studies related to chronic brain inflammation.

CI-1018 is an orally active selective PDE-4 inhibitor, with IC₅₀ values of 1.1 μM, 35.8 μM, and 73.4 μM against hPDE-4, canine PDE-4, and guinea pig PDE-4, respectively. CI-1018 induces iNOS expression and Apoptosis. CI-1018 induces vascular injury, medial necrosis, hemorrhage, edema, thymic atrophy, ketonuria, and weight loss. CI-1018 can be used in research related to asthma, vasculitis, and mesenteric vasculitis/arteriopathy.