ζ-Stat

ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro[1][2].

Signaling Pathways >> Epigenetics >> PKC

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> TGF-beta/Smad >> PKC

aPKC-ζ: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.

[1]. 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.

[2]. 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.