生物活性 | |||
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描述 | 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]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.51mL 0.70mL 0.35mL |
17.53mL 3.51mL 1.75mL |
35.06mL 7.01mL 3.51mL |
参考文献 |
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[2]Suryakant K Niture,et al. Regulation of Nrf2-an update. Free Radic Biol Med. 2014 Jan;66:36-44. |