General description
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.
Biochem/physiol Actions
Cell permeable: no
Primary Target
DNA-PK
Product competes with ATP.
Reversible: yes
Target IC50: 270 nM against DNA-PK
Packaging
Packaged under inert gas
Warning
Toxicity: Carcinogenic / Teratogenic (D)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Knight, Z.A., et al. 2004. Bioorg. Med. Chem.12, 4749.
Willmore, E., et al. 2004. Blood,103, 4659.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51182057
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 260964-5MG
- CAS:
- 404009-46-7
