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SML1415 Sigma-Aldrich

VE-821

≥98% (HPLC)

Synonym: 3-Amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, 3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide, VE821

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Properties

Related Categories ATR, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience,
InChI Key   DUIHHZKTCSNTGM-UHFFFAOYSA-N
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 10 mg/mL, clear
  H2O: 10 mg/mL, clear
storage temp.   −20°C

Description

Application

VE-821 has been used as an inhibitor of ATM- and Rad3-related (ATR) protein in human cancer cells.

Packaging

5, 25 mg in glass bottle

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-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.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis

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Milli-Q® Water Purification Solutions
Protocols & Articles
Peer-Reviewed Papers
15

References

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