KRAS G12C/SOS1 binding kit
KRAS G12C/SOS1 biochemical binding assay
The KRAS WT/SOS1 binding kit is designed to identify KRAS WT/SOS1 inhibitors.
A fast and easy way to identify new inhibitors of KRAS WT / SOS1 protein interactions.
KRAS is a small GTPase implicated in various biological processes, such as cell proliferation, cell survival, and cell metabolism. This proto-oncogene is well known to be mutated in many cancer subtypes, inducing an uncontrolled proliferation and cell metabolism modifications. It thereby contributes to the Warburg effect in cancer cells. Like the majority of small GTPase, KRAS binds to GDP in its inactive form or binds to GTP to switch into the active form. KRAS G12C is one of the most commonly represented mutant forms in cancer, which leads to a permanently active state of KRAS. The Ras guanine nucleotide exchange factor, also called SOS1, is a GEF protein promoting the active form of KRAS. The upregulation of the KRAS / SOS1 interaction leads to cancer phenotypes.
Various compounds known to be KRAS or SOS1 inhibitors were added to the assay. BAY-293, BI-3406, BI-2852, and MRTX-1257 display the right potency and pharmacological ranking, in good correlation with the literature. ARS-1620 and AMG-510, two KRAS G12C selective compounds, had no effect on the assay, confirming that the KRAS WT/SOS1 binding kit is specific to the KRAS WT form.
The two nucleotides GDP and ATP were added to the assay. GDP, a GTP competitor which is well known to bind KRAS WT, displays the right potency, in good correlation with the literature. ATP, a non GTP competitive nucleotide, had no effect on the assay, confirming the specificity of the kit in detecting GTP competitors or KRAS WT / SOS1 inhibitors.
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