ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
Chemical Formula: C₁₀H₅Na₃O₁₀S₃
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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.
- Ratnayake WS, et, al. Oncogenic PKC-ι activates Vimentin during epithelial-mesenchymal transition in melanoma; a study based on PKC-ι and PKC-ζ specific inhibitors. Cell Adh Migr. 2018; 12(5):447-463.
- Islam SMA, et, al. Atypical Protein Kinase-C inhibitors exhibit a synergistic effect in facilitating DNA damaging effect of 5-fluorouracil in colorectal cancer cells. Biomed Pharmacother. 2020 Jan; 121:109665.
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