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.

• 同義詞: DNA-PK Inhibitor II, NU7026, DNA-Dependent Protein Kinase Inhibitor II, 2-(Morpholin-4-yl)-benzo[h]chromen-4-one, LY293646
• 經驗公式（希爾表示法）: C₁₇H₁₅NO₃
• CAS號碼: 154447-35-5
• 分子量：: 281.31
• MDL號碼: MFCD06798345
• 分類程式碼代碼: 12352200

屬性

• 品質等級: 100
• 化驗: ≥95% (HPLC)
• 形狀: crystalline solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 溶解度: DMSO: 2 mg/mL; methanol: 700 μg/mL
• 運輸包裝: ambient
• 儲存溫度: 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 密鑰: KKTZALUTXUZPSN-UHFFFAOYSA-N

描述

一般說明

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.

生化／生理作用

Cell permeable: yes

Primary Target
DNA-PK

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.23 µM against DNA-PK

包裝

Packaged under inert gas

警告

Toxicity: Carcinogenic / Teratogenic (D)

重構

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

其他說明

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.

法律資訊

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3