Nrf2 is a nuclear factor that controls the expression and coordinated induction of a battery of genes that encode detoxifying enzymes, drug transporters, antiapoptotic proteins, and proteasomes[2].
NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential. NK-252 interacts with the domain containing the Nrf2-binding site of Keap1 in vitro binding studies. The administration of NK-252 significantly attenuated the progression of histologic abnormalities in rats[3]. NK-252 could potentiate the antitumor activity of multiple anticancer agent including vincristine (VCR), vinblastine, vindesine and actinomycin D in drug-resistant tumor cells and their parental drug-sensitive tumor cells. NK-252 at 5-10μM almost completely reversed VCR resistance in cultured VCR-resistant P388/VCR cells and at 1-10μM inhibited the photoaffinity labeling by [3H]azidopine of the cell-surface 170,000-molecular-weight P-glycoprotein[4].
NK-252 细胞实验
Cell Line
Concentration
Treated Time
Description
References
P388/VCR cells
5 μg/ml and 10μg/ml
4 days
NK-252 almost completely overcame the cross-resistance to etoposide of P388/VCR cells
Br J Cancer. 1991 Aug;64(2):221-6.
P388/S cells
5μg/ml and 10μg/ml
4 days
NK-252 potentiated the cytotoxic action of etoposide against P388/S cells
Br J Cancer. 1991 Aug;64(2):221-6.
HT29 cells
200 µM
Activate the Nrf2 signaling pathway, reversing oxaliplatin-induced ferroptosis and oxidative stress
Exp Ther Med. 2022 Jun;23(6):394.
NK-252 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
CD2F1 mice
P388/S and P388/VCR leukemia mouse model
Oral
100, 300, 1000 mg/kg
Once daily for 5 days
NK-252 alone showed no antitumour activity in P388/S- and P388/VCR-mice, but significantly extended the survival time when combined with etoposide
搜索
