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KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.

KRA-333 is a potent and selective KRAS agonist th at binds directly to the GTP/GDP binding pocket of KRAS preventing the cleavage of GTP into GDP and caucusing accumulation of activated GTP-KRAS and suppression of cell growth. KRA-333 promotes apoptosis and autophagic cell death of cancer cells and inhibits growth of mutant KRAS lung cancer in xenografts mice model.

[1] Xu K, et al. Small Molecule KRAS Agonist for Mutant KRAS Cancer Therapy [published correction appears in Mol Cancer. 2020 May 20;19(1):93]. Mol Cancer. 2019;18(1):85. Published 2019 Apr 10. DOI:10.1186/s12943-019-1012-4