ζ-Stat trisodium (NSC37044 trisodium) 是一种特异且非典型的 PKC-ζ 的抑制剂，IC50 值为 5 μM。ζ-Stat trisodium 可以减少黑色素瘤细胞系的增殖并诱导细胞凋亡，在体外具有抗肿瘤活性。
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[1][2].
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].
[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.
动态评分
0.0