General description

A cell-permeable disubstituted pyranone compound that acts as a potent and ATP-competitive inhibitor of ATM kinase (IC₅₀ = 13 nM; K_i = 2.2 nM). Displays excellent selectivity over other PIKK family kinases (IC₅₀ = 2.5, 9.3, 16.6 µM for DNA-PK, mTOR, PI 3-K, respectively; IC₅₀ >100 µM for PI 4-K and ATR) and exhibits little activity towards a panel of 60 other kinases even at concentrations as high as 10 µM. Inhibits ATM-dependent cellular protein phosphorylation following ionizing radiation (IR) and sensitizes cells with wild-type ATM, but not mutant ATM, to the cytotoxic effects of IR and DNA-damaging agents.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Pereg, Y., et al. 2005. Proc. Natl. Acad. Sci. USA102, 5056.Lau, A., et al. 2005. Nat. Cell Biol.7, 493.Hickson, I., et al. 2004. Cancer Res.64, 9152.

Packaging

Packaged under inert gas

2 mg in Glass bottle

Physical form

A 10 mM (2 mg/506 µl) solution of ATM Kinase Inhibitor (Cat. No. 118500) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C).

Warning

Toxicity: Irritant (B)