ζ-Stat trisodium (NSC37044 trisodium) is a potent and selective inhibitor of protein kinase C-ζ (PKC-ζ), exhibiting an IC50 of 5 μM. It effectively suppresses the proliferation of melanoma cell lines and promotes apoptosis. Moreover, ζ-Stat trisodium demonstrates notable antitumor activity in vitro.

APKCζ:5 μM (IC50)

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[1]. ζ-Stat (0.1-10 μM; 3 d) significantly decreases cell proliferation of SK-MEL-2 and MeWo upon increasing the concentrations[1]. ζ-Stat (7 or 10 μM; 24-72?h) and 5-FU in combination is able to decrease the viability of LoVo CRC cells by more than 75%[2]. ζ-Stat (5 μM; 3 d) shows a significant diminution of phosphorylated, total PKC-ζ, Bcl-2 and PARP levels, and increases Caspase-3 and cleaved-PARP levels in SK-MEL-2 and MeWo cells[1]. ζ-Stat (5 μM; 1-10 h) does not show significant cytotoxicity on MEL-F-NEO, SK-MEL-2 and MeWo cells[1]. Cell Proliferation Assay[1]Cell Line: MEL-F-NEO, SK-MEL-2 and MeWo cells Concentration: 0.1, 0.5, 1, 2.5, 5, 7.5, 10 μM Incubation Time: 3 days Result: Decreased proliferation by 47.7% for 5 μM in SK-MEL-2 cells and by 50.6% for 5 μM in MeWo cells. Showed significant inhibitions on MEL-F-NEO cells 19.3% (P ≤ 0.05) at 10 μM. Western Blot Analysis[1]Cell Line: SK-MEL-2 and MeWo cells Concentration: 5 μM Incubation Time: 3 days Result: Decreased phosphorylated and total PKC-ζ levels.