DNA-PK Inhibitor V

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.

Cell permeable: no

Primary Target
DNA-PK

Product competes with ATP.

Reversible: yes

Target IC₅₀: 270 nM against DNA-PK

Packaged under inert gas

Toxicity: Carcinogenic / Teratogenic (D)

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

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

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