KRA-533 (NSC112533, KRA533) is a small molecule KRAS agonist that binds the GTP/GDP-binding pocket of KRAS.
KRA-533 activates KRAS in association with growth inhibition of NSCLC cells, directly binds and activates WT and mutant KRAS (G12C, G12D and G13D mutant) in an in vitro cell-free system.
KRA-533 activated exogenous WT and S17A but not K117A KRAS mutant in A549 cells, suggest that the Lys117 hydrogen-bond site is required for KRA-533 to bind or activate KRAS.
KRA-533 induces KRAS activation leading to apoptotic and autophagic cell death in human lung cancer cells.
KRA-533 suppresses mutant KRAS lung cancer in xenograft models.
