ATM/ATR Kinase Inhibitor

Biochem/physiol Actions

Reversible: no

Primary TargetATM/ATR

Product does not compete with ATP.

Target IC₅₀: ~200 nM against ATM and ATR

Cell permeable: yes

General description

A cell-permeable thiourea compound that selectively inhibits the kinase activity of ATM and ATR (IC₅₀ = ~200 nM) without significant effect against other PIKK family members (PI 3-K, mTOR, and DNA-PK) or kinases that are known to phosphorylate p53 (ERK, CK1, Cdk2, JNK, PKC, CAK, Chk1, PKR, and p38). Shown to reverse senescence in human primary BJ and HMEC cells. Unlike LY 294002 (Cat. No. 440202 and 440204), this inhibitor does not interfere with cellular PI 3-K/PDK1/Akt signaling pathway.

A cell-permeable thiourea compound that selectively inhibits the kinase activity of ATM and ATR (IC₅₀ ~ 200 nM) without significant effect against other PIKK family members (PI3K, mTOR, and DNA-PK) or kinases that are known to phosphorylate p53 (ERK, CK1, Cdk2, JNK, PKC, CAK, Chk1, PKR, and p38). Shown to reverse senescence in human primary BJ and HMEC cells. Unlike LY 294002 (Cat. No. 440202 and 440204), this inhibitor does not interfere with cellular PI3K-PDK1-Akt signaling pathway.

Legal Information

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

Other Notes

Goldstein, M., et al. 2008. Toxicol. Appl. Pharmacol.in press.Crescenzi, E., et al. 2008. Clin. Cancer Res.14, 1877.Cruet-Hennequart, S., et al. 2008. DNA Repair7, 582.Won, J., et al. 2006. Nat. Chem. Biol.2, 369. (RETRACTED)

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Irritant (B)