NRAS-G4-ligand-1

NRAS-G4-ligand-1 is a NRAS-G4 binder with K d values of 0.25 μM (AlexaFluor 647-labeled) and 0.932 μM (biotinylated), respectively. NRAS-G4-ligand-1 acts as a translation inhibitor, reduces cancer cell viability, and downregulates NRAS protein levels. NRAS-G4-ligand-1 can be used in the research of melanoma and breast cancer ^[1].

In Vitro, NRAS-G4-ligand-1 (Compound 18) (0-25 μM; 15 min) binds to purified AlexaFluor 647-labeled NRAS-G4 RNA, with a KD of 0.25 μM^[1]. NRAS-G4-ligand-1 (0-12 μM; 120 sec association, 200 sec dissociation) binds to immobilized biotinylated NRAS-G4 RNA with a KD of 0.93 μM^[1]. NRAS-G4-ligand-1 (0-20 μM; 15 min before translation, 90 min in vitro translation) dose-dependently inhibits the translation of the G4-structured NRAS-G4-FL luciferase reporter transcript in rabbit reticulocyte lysate, while exerting no effect on the G4-free NRAS-G4-Del-FL transcript^[1]. NRAS-G4-ligand-1 (0-20 μM; 48 h) induces a moderate (approximately 20%-30%), dose-dependent reduction in NRAS protein levels in MCF-7 and SK-MEL-2 cells at concentrations up to 20 μM^[1]. NRAS-G4-ligand-1 (0-2.5 μM; 48 h) reduces the viability of MCF-7 and SK-MEL-2 cancer cells, with IC₅₀ values of 1.1 μM and 0.9 μM, respectively^[1].

References:
[1]. Balaratnam S, et al. Investigating the NRAS 5' UTR as a target for small molecules. Cell chemical biology. 2023 Jun 15;30(6):643-657.e8.