BRD7398 is a RSK kinase inhibitor that induces insulin expression and differentiation of pancreatic alpha into beta cells. BRD7398 inhibits RSK1, RSK2 and RSK3; IC50 values of 1.5, 2.4 and 1.2 uM, respectively. Treatment of mouse aTC1 cells with BRD7398 induced expression of b-cell markers Pdx1, Pax4, Iapp and Npy and also induced insulin production.
特徴および利点
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KRAS is a regulator of the nutrient stress response in non-small-cell lung cancer (NSCLC). Induction of the ATF4 pathway during nutrient depletion requires AKT and NRF2 downstream of KRAS. The tumor suppressor KEAP1 strongly influences the outcome of activation of