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NK-252

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Chemical Structure| 1414963-82-8 同义名 : -
CAS号 : 1414963-82-8
货号 : A278611
分子式 : C13H11N5O3
纯度 : 99%+
分子量 : 285.258
MDL号 : MFCD28009512
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 30 mg/mL(105.17 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
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
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

[1]Shimozono R, Asaoka Y, et al. Nrf2 activators attenuate the progression of nonalcoholic steatohepatitis-related fibrosis in a dietary rat model. Mol Pharmacol. 2013 Jul;84(1):62-70.

[2]Suryakant K Niture,et al. Regulation of Nrf2-an update. Free Radic Biol Med. 2014 Jan;66:36-44.

[3]Shimozono R, Asaoka Y, Yoshizawa Y, et al. Nrf2 activators attenuate the progression of nonalcoholic steatohepatitis-related fibrosis in a dietary rat model. Mol Pharmacol. 2013. 84(1), 62-70.

[4]Kiue, A. et al. Reversal by Two Dihydropyridine compounds of resistance to multiple anticancer agents in mouse P388 Leukemia in vivo and in vitro. Wiley Online Library. 1990. 81(10), 1057-1064.