ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC 50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis , and has 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. ζ-Stat (0.1-10 µM; 3 d) significantly decreases cell proliferation of SK-MEL-2 and MeWo upon increasing the concentrations. 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%. 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. ζ-Stat (5 µM; 1-10 h) does not show significant cytotoxicity on MEL-F-NEO, SK-MEL-2 and MeWo cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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 AnalysisCell Line: SK-MEL-2 and MeWo cells Concentration: 5 µM Incubation Time: 3 days Result: Decreased phosphorylated and total PKC-ζ levels.
