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Sigma-Aldrich

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.

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Synonym(s):
DNA-PK Inhibitor V, AMA37, Aryl Morpholine Analog 37, 1-(2-Hydroxy-4-morpholin-4-yl-phenyl)-phenyl-methanone
Empirical Formula (Hill Notation):
C17H17NO3
CAS Number:
Molecular Weight:
283.32
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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

storage temp.

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

InChI key

FALILNHGILFDLC-UHFFFAOYSA-N

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

WGK

WGK 1


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