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.

• 同義詞: Eg5 Inhibitor III, Dimethylenastron, 7,7-Dimethyl-4-(3-hydroxyphenyl)-5-oxo-3,4,5,6,7,8-hexahydroquinazolin-2(1H)-thione
• 經驗公式（希爾表示法）: C₁₆H₁₈N₂O₂S
• CAS號碼: 863774-58-7
• 分子量：: 302.39
• MDL號碼: MFCD09264157
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥95% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: white to light yellow
• 溶解度: DMSO: 10 mg/mL; methanol: 5 mg/mL
• 運輸包裝: ambient
• 儲存溫度: 2-8°C
• SMILES 字串: 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 密鑰: RUOOPLOUUAYNPY-UHFFFAOYSA-N

描述

一般說明

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.

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.

生化／生理作用

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

包裝

Packaged under inert gas

警告

Toxicity: Harmful (C)

重構

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

其他說明

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

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
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable