260961

DNA-PK Inhibitor II

The DNA-PK Inhibitor II, also referenced under CAS 154447-35-5, controls the biological activity of DNA-PK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinônimo(s): DNA-PK Inhibitor II, NU7026, DNA-Dependent Protein Kinase Inhibitor II, 2-(Morpholin-4-yl)-benzo[h]chromen-4-one, LY293646
• Fórmula empírica (Notação de Hill): C₁₇H₁₅NO₃
• Número CAS: 154447-35-5
• Peso molecular: 281.31
• Número MDL: MFCD06798345
• Código UNSPSC: 12352200

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• forma: crystalline solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• solubilidade: DMSO: 2 mg/mL; methanol: 700 μg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C
• InChI: 1S/C17H15NO3/c19-15-11-16(18-7-9-20-10-8-18)21-17-13-4-2-1-3-12(13)5-6-14(15)17/h1-6,11H,7-10H2
• chave InChI: KKTZALUTXUZPSN-UHFFFAOYSA-N

Descrição

Descrição geral

A cell-permeable benzochromenone compound that acts as a potent, specific, reversible, and ATP-competitive inhibitor of DNA-PK with an IC₅₀ of 0.23 µM. It is highly selective towards DNA-PK over PI3K-related kinases (IC₅₀ = 13 µM for PI 3-K and >100 µM for ATM and ATR) and has no effect on PARP-1. Inhibits DNA-PK-mediated, but not PARP-1-mediated, cellular DNA DSB (double strand break) repair and PLDR (potentially lethal damage recovery) following IR (ionizing radiation). Shown to sensitize both proliferating and quiescent cells to IR.

A cell-permeable, potent, specific, reversible, and ATP-competitive inhibitor of DNA-PK (IC₅₀ = 230 nM). Reported to be highly selective for DNA-PK compared to PI3 K-related kinases (IC₅₀ = 13 µM for PI 3-K and >100 µM for ATM and ATR). Exhibits no inhibitory effect on PARP-1. Shown to inhibit DNA-PK-mediated, but not PARP-1-mediated, cellular DNA double strand break (DSB) repair and potentially lethal damage recovery (PLDR) following ionizing radiation (IR). Also shown to sensitize both proliferating and quiescent cells to IR.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
DNA-PK

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.23 µM against DNA-PK

Embalagem

Packaged under inert gas

Advertência

Toxicity: Carcinogenic / Teratogenic (D)

Reconstituição

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

Outras notas

Willmore, E., et al. 2004. Blood,103, 4659.
Hollick, J.J., et al. 2003. Bioorg. Med. Chem. Lett.13, 3083.
Veuger, S.J., et al. 2003. Cancer Res.63, 6008.
Vlahos, C.J., et al. 1994. J. Biol. Chem.269, 5241.

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