NLS-StAx-h TFA is a selective, cell permeable, stapled peptide Wnt signaling inhibitor with an IC50 of 1.4 μM. NLS-StAx-h TFA efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h TFA shows anti-proliferation of cancer cells[1][2].
NLS-StAx-h (10 μM; 72 h) inhibits proliferation of colorectal cancer cells[1].
NLS-StAx-h (5 and 10 μM; 24 h) inhibits migration of colorectal cancer cells[1].
Cell Proliferation Assay[1]
| Cell Line: | SW-480 and DLD-1 cells |
| Concentration: | 10 μM |
| Incubation Time: | 72 hr |
| Result: | Reduced the viability of both SW-480 and DLD-1 by more than 80%. |
Cell Migration Assay [1]
| Cell Line: | DLD-1 cells |
| Concentration: | 5 and 10 μM |
| Incubation Time: | 24 hr |
| Result: | Resulted in dose-dependent inhibition of wound closure (wound closure: 52% at 5 μM, and 24% at 10 μM). |
[1]. Dietrich L, et al. Cell Permeable Stapled Peptide Inhibitor of Wnt Signaling that Targets β-Catenin Protein-Protein Interactions. Cell Chem Biol. 2017 Aug 17;24(8):958-968.e5.
[2]. Wang Z, et al. Direct targeting of β-catenin in the Wnt signaling pathway: Current progress and perspectives. Med Res Rev. 2021 Jul;41(4):2109-2129.