| Assay Method Information | |
| | K-RAS Inhibition Assay |
| Description: | Table 1: Potency and efficacy of K-RAS inhibition and toxicity of batch1 and 2 compounds. MDCK cells co-expressing GFP-K-RASG12V and mCherry-CAAX were grown on coverslips, treated with 0.1% vehicle (DMSO) or variousconcentrations of drugs (A; batch 1, B; batch 2) for 48 h, and fixed with 4%paraformaldehyde. The coverslips were mounted in mowiol and imaged byconfocal microscopy (Nikon A1) using a 60× objective. Using ImageJ softwarev1.42q, images were converted to 8-bit, and a threshold to a control pixel of eachimage was set. As a measure of K-Ras mislocalization, the fraction of mCherry-CAAX co-localizing with mGFP-K-RASG12V was calculated using a Manderscoefficient plugin downloaded from Wright Cell Image Facility. |
| Affinity data for this assay | |
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