Synonyms: 3-Amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide; 3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide; VE821
Molecular Formula: C18H16N4O3S
Molecular Weight: 368.41
Linear Structural Formula: C18H16N4O3S
MDL Number: MFCD19443686
Purity: >=98% (HPLC)
Storage: -20C
Application: VE-821 has been used as an inhibitor of ATM- and Rad3-related (ATR) protein in human cancer cells.
Biochem Physiol Actions: 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-gamma (Ki of 16 muM, 2.2 muM, >1 muM and 3.9 muM, 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.