NQO1 Inducer

TBE 31 is an orally active Keap1/Nrf2 pathway activator and NQO1 inducer with a D_m value of 1.1 nM for NQO1. TBE 31 binds to cysteine residues of Keap1, inhibits ubiquitination and degradation of Nrf2, thereby activating the expression of ARE-dependent genes. TBE 31 induces cytoprotective enzymes including NQO1 and GST isoforms, promotes Nrf2 accumulation, and upregulates Nrf2-regulated genes related to antioxidation and lipid metabolism. TBE 31 inhibits pro-inflammatory responses, formation of AFB1-DNA adducts, endoplasmic reticulum stress, cell apoptosis (apoptosis), hepatic fibrosis, oxidative stress, and the expression of ChREBP. TBE 31 reduces the number of tumors in a mouse model of ultraviolet-induced skin carcinogenesis. TBE 31 enhances nerve growth factor-induced neurite outgrowth. TBE 31 attenuates LPS-induced serum TNF-α levels and immobility time in mice. TBE 31 can be used in research related to liver cancer, skin cancer, inflammation-related depression, and non-alcoholic steatohepatitis.

Glucocamelinin (GSL 10) is a sulfinyl glucosinolate identified from seeds of Camelina sativa and an upregulator of quinone reductase (NQO1). Glucocamelinin upregulates the activity of phase II detoxifying enzymes, exhibits selective cytotoxic activity against lung cancer cells, and possesses in vitro antioxidant activity. Glucocamelinin can be used in studies related to non-small cell lung cancer.