NK-252

SKU: orb1307958

Description

NK-252 is a potent small molecule activator of the Nrf2 pathway. It is utilized in research to study oxidative stress response mechanisms in both cellular and animal models, supporting investigations in fields like neuroprotection and inflammation.

Research Area

Immunology & Inflammation, Metabolism Research

Key Properties

• CAS Number: 1414963-82-8
• MW: 285.26
• Purity: 99.32% (May vary between batches)
• Formula: C₁₃H₁₁N₅O₃
• SMILES: O=C(NCc1ccccn1)Nc1nnc(o1)-c1ccco1
• Target: Nrf2,Reductase
• Solubility: DMSO:29 mg/mL (101.66 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.01 mM)

Bioactivity

• 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. CDAA diet-fed rats showed a nearly 20-fold increase in liver fibrosis area compared to rats on a normal diet (naive), which was significantly reduced by 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. Similarly, oral administration of NK-252 with Etoposide significantly prolonged the lifespan of P388/S inoculated mice, showing an improved therapeutic outcome compared to using Etoposide by itself.
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• 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NK 252, NK252, NK-252, Keap1-Nrf2, inhibit, Nrf2, Inhibitor

Compound Identifiers

PubChem CID

71618700