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NK 252

Catalog No.
C5715
Nrf2 activator
Grouped product items
SizePriceStock Qty
5mg
$91.00
Ship with 5-10 days
10mg
$165.00
Ship with 5-10 days
25mg
$371.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

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Background

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.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt285.3
Cas No.1414963-82-8
FormulaC13H11N5O3
Solubility≤14mg/ml in DMSO;20mg/ml in dimethyl formamide
Chemical NameN-[5-(2-furanyl)-1,3,4-oxadiazol-2-yl]-N'-(2-pyridinylmethyl)-urea
SDFDownload SDF
Canonical SMILESO=C(NC1=NN=C(C2=CC=CO2)O1)NCC3=CC=CC=N3
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Quality Control

Quality Control & MSDS

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Chemical structure

NK 252