| Assay Method Information | |
| | K-RAS Inhibition Assay |
| Description: | Table 3: Potency and efficacy K-RAS inhibition and toxicity of batch 3 compounds. MDCK cells co-expressing GFP-K-RASG12V and mCherry-CAAX were grown on coverslips,treated with 0.1% vehicle (DMSO) or various concentrations of batch 3 compounds for 48 h, and fixed with 4% paraformaldehyde. The coverslips were mounted in mowiol and imaged by confocal microscopy (Nikon A1) using a 60× objective. UsingImageJ software v1.42q, images were converted to 8-bit, and a threshold to acontrol pixel of each image was set. As a measure of K-Ras mislocalization, thefraction of mCherry-CAAX co-localizing with mGFP-K-RASG12V was calculatedusing a Manders coefficient plugin downloaded from Wright Cell Image Facility.Dose-response curves (three parameter fitting) were plotted using GraphPad Prismand IC50 and Emax values were calculated using the software. |
| Affinity data for this assay | |
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