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经验公式(希尔记法):
C17H17NO3
化学文摘社编号:
分子量:
283.32
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
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.
SMILES string
N3(CCOCC3)c1cc(c(cc1)C(=O)c2ccccc2)O
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
InChI key
FALILNHGILFDLC-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 5 mg/mL
shipped in
ambient
Quality Level
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
DNA-PK
Product competes with ATP.
Reversible: yes
Target IC50: 270 nM against DNA-PK
Packaging
Packaged under inert gas
Preparation Note
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.
Willmore, E., et al. 2004. Blood,103, 4659.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
存储类别
11 - Combustible Solids
wgk
WGK 1
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