118501

ATM/ATR Kinase Inhibitor

The ATM/ATR Kinase Inhibitor, also referenced under CAS 905973-89-9, controls the biological activity of ATM/ATR Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 別名: ATM/ATR Kinase Inhibitor, CGK 733
• 実験式（ヒル表記法）: C₂₃H₁₈Cl₃FN₄O₃S
• CAS番号: 905973-89-9
• 分子量: 555.84
• MDL番号: MFCD09038682
• UNSPSCコード: 12352200
• NACRES: NA.77

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: pale yellow
• 溶解性: DMSO: 5 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: Fc1c(cc(cc1)NC(=S)NC(NC(=O)C(c3ccccc3)c2ccccc2)C(Cl)(Cl)Cl)[N+](=O)[O-]
• InChI: 1S/C23H18Cl3FN4O3S/c24-23(25,26)21(30-22(35)28-16-11-12-17(27)18(13-16)31(33)34)29-20(32)19(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-13,19,21H,(H,29,32)(H2,28,30,35)
• InChI Key: HLCDNLNLQNYZTK-UHFFFAOYSA-N

詳細

詳細

A cell-permeable thiourea compound that selectively inhibits the kinase activity of ATM and ATR (IC₅₀ = ~200 nM) without significant effect against other PIKK family members (PI 3-K, mTOR, and DNA-PK) or kinases that are known to phosphorylate p53 (ERK, CK1, Cdk2, JNK, PKC, CAK, Chk1, PKR, and p38). Shown to reverse senescence in human primary BJ and HMEC cells. Unlike LY 294002 (Cat. No. 440202 and 440204), this inhibitor does not interfere with cellular PI 3-K/PDK1/Akt signaling pathway.

A cell-permeable thiourea compound that selectively inhibits the kinase activity of ATM and ATR (IC₅₀ ~ 200 nM) without significant effect against other PIKK family members (PI3K, mTOR, and DNA-PK) or kinases that are known to phosphorylate p53 (ERK, CK1, Cdk2, JNK, PKC, CAK, Chk1, PKR, and p38). Shown to reverse senescence in human primary BJ and HMEC cells. Unlike LY 294002 (Cat. No. 440202 and 440204), this inhibitor does not interfere with cellular PI3K-PDK1-Akt signaling pathway.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
ATM/ATR

Product does not compete with ATP.

Reversible: no

Target IC₅₀: ~200 nM against ATM and ATR

包装

Packaged under inert gas

警告

Toxicity: Irritant (B)

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

Goldstein, M., et al. 2008. Toxicol. Appl. Pharmacol.in press.
Crescenzi, E., et al. 2008. Clin. Cancer Res.14, 1877.
Cruet-Hennequart, S., et al. 2008. DNA Repair7, 582.
Won, J., et al. 2006. Nat. Chem. Biol.2, 369. (RETRACTED)

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
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable