260962

DNA-PK Inhibitor III

The DNA-PK Inhibitor III, also referenced under CAS 404009-40-1, controls the biological activity of DNA-PK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 別名: DNA-PK Inhibitor III, IC86621, 1-(2-Hydroxy-4-morpholin-4-yl-phenyl)ethanone
• 実験式（ヒル表記法）: C₁₂H₁₅NO₃
• CAS番号: 404009-40-1
• 分子量: 221.25
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 5 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• InChI: 1S/C12H15NO3/c1-9(14)11-3-2-10(8-12(11)15)13-4-6-16-7-5-13/h2-3,8,15H,4-7H2,1H3
• InChI Key: YHKSBKQXCWHTQL-UHFFFAOYSA-N

詳細

詳細

A cell-permeable aryl-morpholino compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC₅₀ = 120 nM) and PI 3-Kinase catalytic subunit p110β (IC₅₀ = 135 nM). It inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC₅₀ = 68 µM) and enhances DSB-induced antitumor activity both in vitro and in vivo, while exhibiting no cytotoxic effects (up to 50 µM) in the absence of DSBs. It inhibits PI 3-K p110α, p110γ, and p110δ only at much higher concentrations (IC₅₀ = 1.4, 0.88, and 1.0 µM, respectively) and exhibits no effect against a panel of several other kinases, including, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12, even at concentrations as high as 100 µM.

A cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC₅₀ = 0.12 µM) and the PI-3 kinase catalytic subunit p110β (IC₅₀ = 0.135 µM). It inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC₅₀ = 68 µM) and enhances DSB-induced anti-tumor activity both in vitro and in vivo. Exhibits no cytotoxic effects (up to 50 µM) in the absence of DSBs. It inhibits PI3K p110α, p110γ, and p110δ only at much higher concentrations (IC₅₀ = 1.4 µM, 880 nM, and 1 µM, respectively) and does not inhibit a panel of several other kinases, including, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12, even at concentrations as high as 100 µM.

生物化学的／生理学的作用

Cell permeable: yes

Product competes with ATP.

Reversible: yes

Target IC₅₀: 120 nM against DNA-PK

包装

Packaged under inert gas

警告

Toxicity: Carcinogenic / Teratogenic (D)

その他情報

Kashishian, A., et al. 2004. Mol. Cancer Ther.2, 1257.
Willmore, E., et al. 2004. Blood,103, 4659.

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