Quinone Reductase Inhibitor

Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC₅₀s of 0.37 and 19.42 μM, respectively.

ES 936 is a potent and specific NQO1 inhibitor. ES 936 inhibits the growth of MIA PaCa-2 and BxPC-3 cells, with IC₅₀ values of 108 nM and 365 nM, respectively. ES936 significantly inhitbits the growth rate of MIA PaCa-2 xenograft tumors in mice. ES 936 can be used for the study of pancreatic cancer.

Casimiroin is a QR2 and Aromatase inhibitor, with an IC₅₀ of 54.1 μM against QR2 and an IC₅₀ of 3.92 μM against aromatase. Casimiroin exhibits antimutagenic activity and inhibits DMBA (HY-W011845)-induced mutations in Salmonella typhimurium. Casimiroin suppresses DMBA-induced precancerous lesions in mouse mammary organ cultures. Casimiroin can be used in breast cancer-related research.

Tretazicar (CB 1954), an antitumor proagent, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1).

FH1 (NSC 12407) is a NQO2 inhibitor with hepatoprotective effects. FH1 enhances hepatocyte function and promotes differentiation of induced pluripotent stem (iPS)-derived hepatocytes to a more mature phenotype and maturation of well-differentiated hepatocyte-like cell (iHeps) cultures. FH1 protects against Acetaminophen (HY-66005)-induced hepatotoxicity in both embryos and adult zebrafish.

Ginsenoside Rh3 is a bacterial metabolite of Ginsenoside Rg5. Ginsenoside Rh3 treatment in human retinal cells induces Nrf2 activation.

KP372-1 is an Akt inhibitor that inhibits proliferation and induces apoptosis and anoikis. KP372-1 is also an NQO1 redox cycling agent that causes DNA damage (including DNA breakage) by generating ROS. KP372-1 can be used in cancer research (such as head and neck squamous cell carcinoma (HNSCC) and pancreatic cancer).

Deoxynyboquinone, an excellent NQO1 substrate, is a potent antineoplastic agent. Deoxynyboquinone induces apoptosis in cancer cell lines. Deoxynyboquinone kills cancer cells through oxidative stress and reactive oxygen species (ROS) formation.

Dehydroglyasperin C, a isoflavone, is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C has antioxidant, neuroprotective, cancer chemopreventive, and anti-inflammatory activities.

Bisindolylmaleimide III is a protein kinase C (PKC) inhibitor with IC₅₀ values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III also exhibits inhibitory activity against other off-targets, with IC₅₀ values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its K_i for NQO2 is 16.5 μM. Bisindolylmaleimide III selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III can be used in studies of signal transduction and colorectal cancer.

Diminutol is an inhibitor for NADP-dependent quinone oxidoreductase (NQO1), that is involved in microtubule morphogenesis and cell devision.

NQO1 Human Pre-designed siRNA Set A contains three designed siRNAs for NQO1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Nqo1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Nqo1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Keap1-IN-1 (Compound 27) is the inhibitor for Keap1, that covalently modifys the Cys151 site in the BTB domain of KEAP1, and interfers with the interaction between Keap-Nrf. Keap1-IN-1 upregulates the mRNA expression of the antioxidant stress element (ARE)-dependent gene NQO1 with an EC₅₀ of 160 nM. Keap1-IN-1 exhibits cytotoxicity in cell U2OS with an EC₅₀ of 527 nM.

IP-DNQ is an efficient NQO1 dependent cytotoxic agent. IP-DNQ has a potent killing effect on MCF-7 cells (IC50 = 0.18 µM). IP-DNQ can be used for cancer research.

PRL-295 is an orally active inhibitor targeting Keap1-Nrf2 interaction. PRL-295 increases the thermal stability of Keap1 and disrupts its interaction with Nrf2, thereby activating the Nrf2-dependent transcriptional target NAD(P)H:quinone oxidoreductase 1 (NQO1). PRL-295 protects against Acetaminophen (HY-66005)-induced liver injury in mice.

Nrf2 activator-27 is a Nrf2 activator with anti-inflammatory activity. Nrf2 activator-27 increases the expression level of Nrf2, promotes its nuclear translocation, and upregulates the downstream target proteins HO-1 and NQO1. Nrf2 activator-27 reduces the production of NO, TNF-α, IL-1β and IL-6 in LPS-stimulated macrophages. Nrf2 activator-27 can be used for the research of inflammation-related diseases.

Bisindolylmaleimide III hydrochloride is a protein kinase C (PKC) inhibitor with IC₅₀ values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III hydrochloride also exhibits inhibitory activity against other off-targets, with IC₅₀ values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its K_i for NQO2 is 16.5 μM. Bisindolylmaleimide III hydrochloride selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III hydrochloride can be used in studies of signal transduction and colorectal cancer.

Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model.

NSC 645827 is an inhibitor for NAD(P)H: quinone oxidoreductase 1 (NQO1) with an IC₅₀ of 0.7 μM.