| NK 252Nrf2 activator |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.00%
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- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 1414963-82-8 | SDF | Download SDF |
| Chemical Name | N-[5-(2-furanyl)-1,3,4-oxadiazol-2-yl]-N"-(2-pyridinylmethyl)-urea | ||
| Canonical SMILES | O=C(NC1=NN=C(C2=CC=CO2)O1)NCC3=CC=CC=N3 | ||
| Formula | C13H11N5O3 | M.Wt | 285.3 |
| Solubility | ≤14mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
NK 252 is an Nrf2 activator [1][2].
Nuclear factor-erythroid-2-related factor 2 (Nrf2), a transcription factor that activates antioxidant response elements (AREs), plays a central role in stimulating expression of various antioxidant-associated genes in the cellular defense against oxidative stress. Keap1 is a cytosolic repressor of Nrf2 that retains Nrf2 in the cytoplasm [1].
NK 252 is an Nrf2 activator that interacts directly with the domain containing the Nrf2-binding site of Keap1. In Huh-7.5 cells, NK 252 activated the NQO1-ARE in a dose-dependent way, suggesting NK-252 has potential as Nrf2 activator in hepatic cells. NK-252 also protected Huh-7 cells against H2O2-induced cytotoxicity [1]. NK-252 was effective not only in circumventing the drug resistance, but also in potentiating the action of antitumor drugs against drug-sensitive tumors [2].
In nonalcoholic steatohepatitis (NASH) model rats, NK-252 decreased fibrosis scores and significantly reduced liver fibrosis area in a dose-dependent way. NK-252 also significantly reduced plasma ALT levels and plasma AST levels, suggesting the hepatoprotective effects of NK-252. NK-252 increased NQO1 gene expression and exhibited antioxidant property in the livers of rats. NK-252 reduced fibrogenic gene expression and inhibited further progression of established fibrosis [1].
References:[1]. 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 Jul;84(1):62-70.[2]. Kiue A, Sano T, Naito A, et al. Reversal by two dihydropyridine compounds of resistance to multiple anticancer agents in mouse P388 leukemia in vivo and in vitro. Jpn J Cancer Res. 1990 Oct;81(10):1057-64.
