260961

DNA-PK Inhibitor II

The DNA-PK Inhibitor II, also referenced under CAS 154447-35-5, controls the biological activity of DNA-PK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(e): DNA-PK Inhibitor II, NU7026, DNA-Dependent Protein Kinase Inhibitor II, 2-(Morpholin-4-yl)-benzo[h]chromen-4-one, LY293646
• Empirische Formel (Hill-System): C₁₇H₁₅NO₃
• CAS-Nummer: 154447-35-5
• Molekulargewicht: 281.31
• MDL-Nummer: MFCD06798345
• UNSPSC-Code: 12352200

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: crystalline solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Löslichkeit: DMSO: 2 mg/mL; methanol: 700 μg/mL
• Versandbedingung: ambient
• Lagertemp.: 2-8°C
• InChI: 1S/C17H15NO3/c19-15-11-16(18-7-9-20-10-8-18)21-17-13-4-2-1-3-12(13)5-6-14(15)17/h1-6,11H,7-10H2
• InChIKey: KKTZALUTXUZPSN-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
DNA-PK

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.23 µM against DNA-PK

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Carcinogenic / Teratogenic (D)

Rekonstituierung

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

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3