VE-821 has been used as an inhibitor of ATM- and Rad3-related (ATR) protein in human cancer cells.[1]
Biochem/physiol Actions
VE-821 is a ATP-competitive inhibitor of ATR.
VE-821 is a potent ATP-competitive inhibitor of the DNA damage response (DDR) kinase Ataxia telangiectasia-mutated (ATM) and ATM- and Rad3-related (ATR) with a Ki of 13 nM. VE-821 has minimal cross-reactivity against the related PIKKs ATM, DNA-dependent protein kinase (DNA-PK), mTOR and PI3-kinase-γ (Ki of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively) and against a large panel of unrelated protein kinases. VE-821 used alone caused death in a large fraction of cancer cell populations and also showed strong synergy with genotoxic agents. VE-821 increased sensitivity of cells to radiation and also sensitized cancer cells to a variety of chemotherapeutic agents.
Other Notes
VE-821 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the VE-821 probe summary on the Chemical Probes Portal website.
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