5.06384

BLM Helicase Inhibitor, ML216

• 別名: BLM Helicase Inhibitor, ML216, 1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea, ML-216, ML-216, 1-(4-Fluoro-3-(trifluoromethyl)phenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea
• 実験式（ヒル表記法）: C₁₅H₉F₄N₅OS
• CAS番号: 1430213-30-1
• 分子量: 383.32
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥97% (HPLC)
• 品質水準: 100
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: orange
• 溶解性: DMSO: 10 mg/mL
• 保管温度: 2-8°C

詳細

詳細

A cell-permeable pyridinyl-thiadiazolylurea compound that selectively blocks Bloom′s syndrome protein (BLM) helicase activity of both full-length as well as truncated BLM^636-1298 forms (IC₅₀ = 2.98 and 0.97 µM, respectively). Competes with and reversibly blocks DNA binding to BLM. However, the inhibition appears to be non-competitive with respect to ATP. Exhibits anti-proliferative activity in cells expressing BLM, but not in those lacking BLM. Induces sister chromatid exchanges (SCEs) and enhances the sensitivity of BLM containing PSNF5 cells to aphidicolin (>Cat. No. 178273) without affecting PSNG13 cells that are devoid of BLM. Displays favorable microsomal (T_1/2 >1.2 h) and plasma stability (~100% at 5 h).

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
BLM

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

その他情報

Rosenthal, A.S., et al. 2013. Bioorg. Med. Chem. Lett. 23, 5660.
Nguyen, G.H., et al. 2013. Chem. Biol.20, 55.

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