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.

• 別名: DNA-PK Inhibitor II, NU7026, DNA-Dependent Protein Kinase Inhibitor II, 2-(Morpholin-4-yl)-benzo[h]chromen-4-one, LY293646
• 実験式（ヒル表記法）: C₁₇H₁₅NO₃
• CAS番号: 154447-35-5
• 分子量: 281.31
• MDL番号: MFCD06798345
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: crystalline solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 溶解性: DMSO: 2 mg/mL; methanol: 700 μg/mL
• 輸送温度: ambient
• 保管温度: 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
• InChI Key: KKTZALUTXUZPSN-UHFFFAOYSA-N

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
DNA-PK

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.23 µM against DNA-PK

包装

Packaged under inert gas

警告

Toxicity: Carcinogenic / Teratogenic (D)

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3