nqo 1

NQO1 substrate is a highly potent NQO1 substrate with potential antitumor activity for leukemia research.

NQO1 inducer 1 (Compound 20) is a potent inducer of NQO1 with a CD value of 3 μM. It acts as a promising antioxidant, making it suitable for studies involving redox regulation.

Dicoumarol (Dicumarol) is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicoumarol is a competitive inhibitor of vitamin K epoxidereductase; thus, it inhibits vitamin K recycling and causes depletion of active vitamin K in blood. This prevents the formation of the active form of prothrombin and several other coagulant enzymes, and inhibits blood clotting.

KL1333 (NQO1 activator 1) enhances energy metabolism and mitochondrial dysfunction in MELAS fibroblasts. Elevated NAD+ levels trigger the activation of SIRT1 and AMPK, and subsequently activates PGC-1α. NQO1 activator 1 is an orally available NAD+ modulator. It reacts with NAD(P)H: NQO1 as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation.

CB1954(Tretazicar (NSC-115829)), an anticancer prodrug, is activated by NAD(P)H quinone oxidoreductase 2. It is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent.

2-HBA, a synthetic analog of curcumin, is an indirect inducer of enzymes that catalyze detoxification reactions through the Keap1-Nrf2-ARE pathway.

NQO2-IN-1, a resveratrol analog, is a potent quinone oxidoreductase 2 (NQO2) inhibitor (IC50=95 nM) with antitumor potential through the generation of ROS and up-regulation of DR5 (death receptor 5) to reverse trial resistance and promote apoptosis.

NQO2 activator-1 (Compound 1d) is a selective NQO2 activator that enhances NQO2 activity by 20.89% at a concentration of 10μM. It strongly inhibits the activation of the NLRP3 inflammasome and is applicable to research in inflammatory and immune disorders, such as rheumatoid arthritis.

Antitumor agent-195 (compound 16c) is a dual-targeting agent that simultaneously targets STAT3 and NQO1. At a concentration of 1 μM, it significantly inhibits the phosphorylation of STAT3 at the Tyr705 site and effectively induces apoptosis in MDA-MB-231 and MDA-MB-468 breast cancer cells. As a substrate of NQO1, Antitumor agent-195 markedly increases ROS production, causing severe DNA damage in a dose-dependent manner. It also demonstrates strong antitumor properties in MDA-MB-231 xenograft models.

4-Nitroquinoline 1-oxide (4-NQO) is a chemical carcinogen that induces mutations in bacteria, fungi, and animals through the formation of large amounts of purine adducts.

ICy-Q, a near-infrared (NIR) reagent activated by quinone oxidoreductase 1 (NQO-1), interacts with NQO-1 to yield the reduced product ICy-OH. This derivative selectively triggers pyroptosis and resultant death in pancreatic cancer cells. Moreover, ICy-Q serves as a valuable instrument for the expedited and precise diagnosis of intraoperative pathological sections [1].