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.

• Sinônimo(s): ATM/ATR Kinase Inhibitor, CGK 733
• Fórmula empírica (Notação de Hill): C₂₃H₁₈Cl₃FN₄O₃S
• Número CAS: 905973-89-9
• Peso molecular: 555.84
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: pale yellow
• solubilidade: DMSO: 5 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 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)
• chave InChI: HLCDNLNLQNYZTK-UHFFFAOYSA-N

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
ATM/ATR

Product does not compete with ATP.

Reversible: no

Target IC₅₀: ~200 nM against ATM and ATR

Embalagem

Packaged under inert gas

Advertência

Toxicity: Irritant (B)

Reconstituição

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

Outras notas

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)

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable