ζ-Stat

Chemical Properties

1-Hydroxynaphthalene-3,6,8-trisulfonic acid [3316-02-7]. (8-hydroxynaphthalene-1,3,6-trisulfonic acid), oxy Koch acid, C10H8O10S3, Mr 384.3, and its alkali-metal salts are readily soluble in water. Amination at 170℃ gives 1-aminonaphthalene-3,6,8-trisulfonic acid. Diazo coupling takes place in the 2-position.

Production Methods

1-Aminonaphthalene-3,6,8-trisulfonic acid is heated with dilute sulfuric acid at 180℃ under pressure for 20 h. After the mixture is run into excess sodium hydroxide solution, ammonia is removed by heating and the total liquor is used directly for the production of chromotropic acid by caustic fusion.

Biological Activity

ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor with IC50 of 5 μM. ζ-Stat reduces proliferation and induces apoptosis in melanoma cell lines, with antitumor activity in vitro.

in vitro

ζ-Stat (0.1-20 μM) shows only 13% inhibition on PKC-ι at 20 μM, but shows a significant inhibition on PKC-ζ as 51% at 5 μM level.

target

aPKC-ζ < span> 5 μM (IC 50 )