Quinone Reductase Substrate

KL1333, a derivative of β-lapachone, is an orally available NAD+ modulator. KL1333 reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation. KL1333 improves energy metabolism and mitochondrial dysfunction in MELAS fibroblasts. KL1333 protects against Cisplatin-induced ototoxicity in mouse cochlear cultures.

Isobutyl-deoxynyboquinone (IB-DNQ) is a selective substrate for NAD(P)H:quinone oxidoreductase (NQO1). Isobutyl-deoxynyboquinone can be used for the research of anticancer.

NQO1 substrate acts as an efficient NQO1 substrate and may be a new option for the treatment of NQO1-overexpresssing drug-resistant NSCLC.

Pronqodine A is an Indoleamine 2,3-Dioxygenase (IDO) inhibitor, with an IC₅₀ of 131.5 nM. Pronqodine A inhibits bradykinin-induced release of PGE2, 6-keto-prostaglandin F_1α, PGD2 and induces the production of reactive oxygen species (ROS) in human synovial sarcoma SW982 cells. Pronqodine A is a good substrate for human quinone reductase NQO1. Pronqodine A can be used for the study of inflammation.

Antitumor agent-67 (compound 3) is a potent antitumor agent. Antitumor agent-67 has highly selective toxicity to cancer cells and lower damage to normal cells. Antitumor agent-67 can be activated by NQO1 and effectively liberate podophyllotoxin and kill tumor cells. Antitumor agent-67 significantly suppresses cancer growth in HepG2 xenograft models without obvious toxicity.

SHN7 is a selective HDAC1/HDAC6 inhibitor, NQO1 substrate and ROS inducer, with an IC₅₀ of 30 nM against HDAC1 and an IC₅₀ of 10 nM against HDAC6. SHN7 inhibits STAT3 with a K_d of 8.9 μM. SHN7 arrests the cell cycle at the G2/M phase and induces Apoptosis. SHN7 exhibits anti-tumor effects in triple-negative breast cancer (TNBC) xenograft models. SHN7 can be used for the research of triple-negative breast cancer.

Nampt-IN-8 (Compound 10d) is an NAMPT inhibitor with an IC₅₀ of 0.183 μM. Nampt-IN-8 is also a relatively good NQO1 substrate. Nampt-IN-8 induces cell apoptosis and ROS.