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260961 Millipore

DNA-PK Inhibitor II - CAS 154447-35-5 - Calbiochem

DNA-PK Inhibitor II, CAS 154447-35-5, is a cell-permeable, potent, specific, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 230 nM).

Synonym: NU7026, DNA-Dependent Protein Kinase Inhibitor II, 2-(Morpholin-4-yl)-benzo[h]chromen-4-one, LY293646, NU7026, DNA-Dependent Protein Kinase Inhibitor II, 2-(Morpholin-4-yl)-benzo[h]chromen-4-one, LY293646

  • CAS Number 154447-35-5

  • Empirical Formula (Hill Notation) C17H15NO3

  • Molecular Weight 281.31

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Properties

Related Categories Biochemicals and Reagents, Cell Biology, Cell Signaling and Neuroscience, DNA-dependent protein kinase (DNA-PK), Kinase/Phosphatase Biology,
packaging   5 mg in Plastic ampoule (260961-5MG)
form   crystalline solid
mfr. no.   Calbiochem
shipped in   ambient
solubility   DMSO: 2 mg/mL
  methanol: 700 μg/mL
storage condition   OK to freeze
  protect from light
purity   ≥95% by HPLC
storage conditions   +2C to +8C

Description

Biochem/physiol Actions

Cell permeable: yes

Primary Target
DNA-PK

Product competes with ATP.

Reversible: yes

Target IC50: 0.23 µM against DNA-PK

General description

A cell-permeable benzochromenone compound that acts as a potent, specific, reversible, and ATP-competitive inhibitor of DNA-PK with an IC50 of 0.23 µM. It is highly selective towards DNA-PK over PI3K-related kinases (IC50 = 13 µM for PI 3-K and > 100 µM for ATM and ATR) and has no effect on PARP-1. Inhibits DNA-PK-mediated, but not PARP-1-mediated, cellular DNA DSB (double strand break) repair and PLDR (potentially lethal damage recovery) following IR (ionizing radiation). Shown to sensitize both proliferating and quiescent cells to IR.

A cell-permeable, potent, specific, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 230 nM). Reported to be highly selective for DNA-PK compared to PI3 K-related kinases (IC50 = 13 µM for PI 3-K and > 100 µM for ATM and ATR). Exhibits no inhibitory effect on PARP-1. Shown to inhibit DNA-PK-mediated, but not PARP-1-mediated, cellular DNA double strand break (DSB) repair and potentially lethal damage recovery (PLDR) following ionizing radiation (IR). Also shown to sensitize both proliferating and quiescent cells to IR.

Other Notes

Willmore, E., et al. 2004. Blood,103, 4659.
Hollick, J.J., et al. 2003. Bioorg. Med. Chem. Lett.13, 3083.
Veuger, S.J., et al. 2003. Cancer Res.63, 6008.
Vlahos, C.J., et al. 1994. J. Biol. Chem.269, 5241.

Packaging

5 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

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

Warning

Carcinogenic / Teratogenic (D)

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.

Documents

Certificate of Analysis

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Protocols & Articles
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