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.
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所有图片(1)
别名:
Eg5 Inhibitor III, Dimethylenastron, 7,7-Dimethyl-4-(3-hydroxyphenyl)-5-oxo-3,4,5,6,7,8-hexahydroquinazolin-2(1H)-thione
经验公式（希尔记法）:
C16H18N2O2S
推荐产品
质量水平
检测方案
≥95% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
light yellow
溶解性
DMSO: 10 mg/mL
methanol: 5 mg/mL
运输
ambient
储存温度
2-8°C
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
一般描述
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
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)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Liu, M., et al. 2006. J. Biol Chem.in press.
Gartner, M., et al. 2005. Chembiochem6, 1173.
Gartner, M., et al. 2005. Chembiochem6, 1173.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Stephen DiGiuseppe et al.
Proceedings of the National Academy of Sciences of the United States of America, 113(22), 6289-6294 (2016-05-18)
During the entry process, the human papillomavirus (HPV) capsid is trafficked to the trans-Golgi network (TGN), whereupon it enters the nucleus during mitosis. We previously demonstrated that the minor capsid protein L2 assumes a transmembranous conformation in the TGN. Here
Roshan L Shrestha et al.
The Journal of cell biology, 220(4) (2021-02-24)
Chromosomal instability (CIN) is a hallmark of many cancers. Restricting the localization of centromeric histone H3 variant CENP-A to centromeres prevents CIN. CENP-A overexpression (OE) and mislocalization have been observed in cancers and correlate with poor prognosis; however, the molecular
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