NK 252
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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 285.3 |
Cas No. | 1414963-82-8 |
Formula | C13H11N5O3 |
Solubility | ≤14mg/ml in DMSO;20mg/ml in dimethyl formamide |
Chemical Name | N-[5-(2-furanyl)-1,3,4-oxadiazol-2-yl]-N'-(2-pyridinylmethyl)-urea |
SDF | Download SDF |
Canonical SMILES | O=C(NC1=NN=C(C2=CC=CO2)O1)NCC3=CC=CC=N3 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
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