324622

Eg5 Inhibitor III, Dimethylenastron

The Eg5 Inhibitor III, Dimethylenastron, also referenced under CAS 863774-58-7, controls the biological activity of Eg5. This small molecule/inhibitor is primarily used for Membrane applications.

• 別名: Eg5 Inhibitor III, Dimethylenastron, 7,7-Dimethyl-4-(3-hydroxyphenyl)-5-oxo-3,4,5,6,7,8-hexahydroquinazolin-2(1H)-thione
• 実験式（ヒル表記法）: C₁₆H₁₈N₂O₂S
• CAS番号: 863774-58-7
• 分子量: 302.39
• MDL番号: MFCD09264157
• 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: white to light yellow
• 溶解性: DMSO: 10 mg/mL; methanol: 5 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: S=C1NC(C3=C(N1)CC(CC3=O)(C)C)c2cc(ccc2)O
• InChI: 1S/C16H18N2O2S/c1-16(2)7-11-13(12(20)8-16)14(18-15(21)17-11)9-4-3-5-10(19)6-9/h3-6,14,19H,7-8H2,1-2H3,(H2,17,18,21)
• InChI Key: RUOOPLOUUAYNPY-UHFFFAOYSA-N

詳細

詳細

A cell-permeable quinazoline-thione compound that acts as a potent, specific, and reversible inhibitor of the microtubule-stimulated ATPase activity of the mitotic motor, Eg5 (IC₅₀ = 200 nM). Exhibits little effect on the ATPase activity of kinesin-1, -4, -7 and -10 and is ~100-fold more potent than Monastrol (Cat. No. 475879). Also inhibits bipolar spindle formation in both HeLa cells and in Xenopus egg extracts and induces cell cycle arrest (~1 µM). Shown to induce mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
Microtubule-stimulated ATPase activity of the mitotic motor

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 200 nM inhibiting the microtubule-stimulated ATPase activity of the mitotic motor, Eg5

包装

Packaged under inert gas

警告

Toxicity: Harmful (C)

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

Liu, M., et al. 2006. J. Biol Chem.in press.
Gartner, M., et al. 2005. Chembiochem6, 1173.

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