118501

ATM/ATR Kinase Inhibitor

The ATM/ATR Kinase Inhibitor, also referenced under CAS 905973-89-9, controls the biological activity of ATM/ATR Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinonimo/i: ATM/ATR Kinase Inhibitor, CGK 733
• Formula empirica (notazione di Hill): C₂₃H₁₈Cl₃FN₄O₃S
• Numero CAS: 905973-89-9
• Peso molecolare: 555.84
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: pale yellow
• Solubilità: DMSO: 5 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• InChI: 1S/C23H18Cl3FN4O3S/c24-23(25,26)21(30-22(35)28-16-11-12-17(27)18(13-16)31(33)34)29-20(32)19(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-13,19,21H,(H,29,32)(H2,28,30,35); HLCDNLNLQNYZTK-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
ATM/ATR

Product does not compete with ATP.

Reversible: no

Target IC₅₀: ~200 nM against ATM and ATR

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Irritant (B)

Ricostituzione

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

Altre note

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)

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable