NK-252 是潜在的Nrf2激活剂，具有很好的Nrf2活化活性。

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

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].

Rats on a choline-deficient L-amino acid–defined (CDAA) diet given OPZ or NK-252 show decreased fibrosis scores compared with CDAA control rats. The effects of NK-252 on both fibrosis score and fibrosis area are dose-dependent[1]. Compared with rats fed a normal control diet (naive) (14.7 and 0.72%, respectively), CDAA control rats display approximately 20-fold augmentation of the liver fibrosis area. This augmentation is also drastically reduced by administration of OPZ or NK-252 (5.80% for OPZ, 6.20% for NK-252_low, and 4.97% for NK-252_high). NK-252 alone has no antitumor effect in P388/S- and P388/VCR-mice. The combination therapy with Etoposide and NK-252 significantly increases the life-span of mice inoculated i.p. with P388/VCR compared with the corresponding survival time with Etoposide alone[2]. The combination therapy of Etoposide with NK-252 administered p.o. significantly increases the life-span of mice inoculated i.p. with P388/S compared with the corresponding therapeutic effects with Etoposide alone.

1414963-82-8

C13H11N5O3

285.26

DMSO:29 mg/mL (101.66 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years