KRAS WT/SOS1 binding kit
KRAS WT/SOS1 biochemical binding assay
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The KRAS WT GTP binding kit is designed to identify KRAS WT / GTP inhibitors.
A fast and easy way to identify new KRAS WT / GTP competitors.
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 GTPases, KRAS binds to GDP in its inactive form or binds to GTP to switch to the active form. KRAS G12C is one of the most commonly present mutant forms in cancer which lead to a permanently active state of KRAS. Identifying new KRAS / GTP competitors is therefore a relevant strategy to control biological processes involved in cancer growth by reducing the KRAS activity, as well as the associated pathways.
GTP-Red reagent Kd | 70nM |
GTP-Red reagent concentration | 50nM |
KRAS GTP binding Standard (GDP) IC50 | 35nM |
KRAS GTP binding Standard Ki | 20.4nM |
Various nucleotides known to be GTP competitors were added to the assay. GDP (assay standard), GTPyS, and GTP displayed the right potency, in good correlation with the literature. ATP, a non-specific nucleotide, and BAY-293, a KRAS/SOS1 inhibitor, had no effect on the assay, confirming the specificity of the kit.
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