260964

DNA-PK Inhibitor V

The DNA-PK Inhibitor V, also referenced under CAS 404009-46-7, controls the biological activity of DNA-PK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinónimos: DNA-PK Inhibitor V, AMA37, Aryl Morpholine Analog 37, 1-(2-Hydroxy-4-morpholin-4-yl-phenyl)-phenyl-methanone
• Fórmula empírica (notación de Hill): C₁₇H₁₇NO₃
• Número de CAS: 404009-46-7
• Peso molecular: 283.32
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Análisis: ≥95% (HPLC)
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: yellow
• solubilidad: DMSO: 5 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• InChI: 1S/C17H17NO3/c19-16-12-14(18-8-10-21-11-9-18)6-7-15(16)17(20)13-4-2-1-3-5-13/h1-7,12,19H,8-11H2
• Clave InChI: FALILNHGILFDLC-UHFFFAOYSA-N

Descripción

Descripción general

A morpholino-benzophenone compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC₅₀ = 270 nM). Inhibits PI 3-K catalytic subunit p110-isozymes at higher concentrations (IC₅₀ = 32 µM, 3.7 µM, 22 µM and ~ 100 µM for α, β, δ and γ, respectively) and weakly inhibits a panel of several other kinases, including, ATM, ATR, CK2, GRK2, mTOR, PI 3KC2α, PI 3KC2β, PI 3KC2γ and PI 4Kβ, even at concentrations as high as 50 µM.

A potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC₅₀ = 0.27 µM). Inhibits the PI 3-K catalytic subunit p110-isozymes at higher concentrations (IC₅₀ = 32 µM, 3.7 µM, 22 µM and ~100 µM for α, β, δ and γ, respectively). Only weakly inhibits a panel of several other kinases, including, ATM, ATR, CK2, GRK2, mTOR, PI-3KC2α, PI-3KC2β, PI-3KC2γ and PI-4Kβ, even at concentrations as high as 50 µM.

Acciones bioquímicas o fisiológicas

Cell permeable: no

Primary Target
DNA-PK

Product competes with ATP.

Reversible: yes

Target IC₅₀: 270 nM against DNA-PK

Envase

Packaged under inert gas

Advertencia

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitución

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

Otras notas

Knight, Z.A., et al. 2004. Bioorg. Med. Chem.12, 4749.
Willmore, E., et al. 2004. Blood,103, 4659.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 1