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NK-252

Catalog No. T16331 CAS 1414963-82-8

NK-252 is a potential activator of Nrf2. It has great Nrf2-activating potential.

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NK-252, CAS 1414963-82-8

Pack Size	Availability	Price/USD
2 mg	In stock	$ 33.00
5 mg	In stock	$ 52.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 150.00
50 mg	In stock	$ 256.00
100 mg	In stock	$ 470.00
1 mL * 10 mM (in DMSO)	In stock	$ 58.00

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Purity: 99.32%

Biological Description

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Description	NK-252 is a potential activator of Nrf2. It has great Nrf2-activating potential.
In vitro	NK-252 shows this effect with higher potency than OPZ based on the fact that the EC2 value (concentration for a 2-fold induction above background), calculated with linear extrapolation from the values above and below the induction threshold, is 20.8 μM for OPZ and 1.36 μM for NK-252. NK-252 has potential as an Nrf2 activator in hepatic cells. The protective effects of OPZ and NK-252 are examined against H2O2-induced cytotoxicity using Huh-7 cells to evaluate their antioxidant properties. The cells treated with OPZ or NK-252 show increased resistance to H2O2-induced cytotoxicity compared with control cells. The luciferase activity in Huh-7.5 cells treated with Oltipraz (OPZ) or NK-252 displays activation of the NAD(P)H quinone oxidoreductase 1 (NQO1)-ARE in a dose-dependent manner. Prototypical Nrf2 activators that include OPZ have been reported to protect microglial cells from H2O2-induced cytotoxicity [1].
In vivo	Rats on a choline-deficient L-amino acid–defined (CDAA) diet that received OPZ or NK-252 exhibited decreased liver fibrosis scores compared to those on the same diet without these compounds. NK-252's impact on fibrosis was dose-dependent[1]. Compared to rats on a normal diet (naive), CDAA diet-fed rats showed a nearly 20-fold increase in liver fibrosis area, which was significantly reduced by OPZ or NK-252 treatments (5.80% for OPZ, 6.20% for NK-252_low, and 4.97% for NK-252_high). Although NK-252 did not show antitumor effects in P388/S- and P388/VCR-mice when used alone, its combination with Etoposide notably enhanced the lifespan of mice with P388/VCR cancer, more than Etoposide alone[2]. Similarly, oral administration of NK-252 with Etoposide significantly prolonged the lifespan of P388/S inoculated mice, showcasing an improved therapeutic outcome compared to using Etoposide by itself.

Molecular Weight	285.26
Formula	C13H11N5O3
CAS No.	1414963-82-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 29 mg/mL (101.66 mM)

References and Literature

1. Shimozono R 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, et al. Enhancement of antitumour activity of etoposide by dihydropyridines on drug-sensitive and drug-resistant leukaemia in mice. Br J Cancer. 1991 Aug;64(2):221-6.

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Keywords

NK-252 1414963-82-8 Immunology/Inflammation Others Nrf2 NK 252 inhibit NK252 Inhibitor Keap1-Nrf2 inhibitor

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