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莫纳托

莫纳托用途

(S)-Monastrol ((+)-Monastrol) 是一种有丝分裂运动蛋白 Eg5 的变构抑制剂,对多种癌细胞系具有抗增殖作用。(S)-Monastrol 抑制哺乳动物单极纺锤体有丝分裂中的细胞。

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莫纳托名称

[ CAS 号 ]:
254753-54-3

[ 中文名 ]:
(4S)-1,2,3,4-四氢-4-(3-羟基苯基)-6-甲基-2-硫代-5-嘧啶羧酸乙酯

[ 英文名 ]:
Monastrol

[英文别名 ]:

F3284-6466
MFCD00813077
monastrol

莫纳托生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 驱动蛋白

信号通路 >> 细胞骨架 >> 驱动蛋白

[参考文献]

[1]. Marques LA, et al. Antiproliferative activity of monastrol in human adenocarcinoma (MCF-7) and non-tumor (HB4a) breast cells. Naunyn Schmiedebergs Arch Pharmacol. 2016 Dec;389(12):1279-1288.

[2]. Mayer TU, et al. Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen. Science. 1999 Oct 29;286(5441):971-4.

莫纳托物理化学性质

[ 密度 ]:
1.34g/cm3

[ 沸点 ]:
441.3ºC at 760mmHg

[ 熔点 ]:
185-185.9ºC(lit.)

[ 分子式 ]:
C₁₄H₁₆N₂O₃S

[ 分子量 ]:
292.35

[ 闪点 ]:
220.7ºC

[ 精确质量 ]:
292.08800

[ PSA ]:
109.72000

[ LogP ]:
1.92380

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
2.13E-08mmHg at 25°C

[ 折射率 ]:
1.648

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: 100 mg/mL

莫纳托安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
22-24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

莫纳托文献

Cytokinetic Failure-induced Tetraploidy Develops into Aneuploidy, Triggering Skin Aging in Phosphovimentin-deficient Mice.

J. Biol. Chem. 290 , 12984-98, (2015)

Tetraploidy, a state in which cells have doubled chromosomal sets, is observed in ∼20% of solid tumors and is considered to frequently precede aneuploidy in carcinogenesis. Tetraploidy is also detecte...

Loop 5-directed compounds inhibit chimeric kinesin-5 motors: implications for conserved allosteric mechanisms.

J. Thorac. Cardiovasc. Surg. 286 , 6201-10, (2011)

The human Eg5 (HsEg5) protein is unique in its sensitivity to allosteric agents even among phylogenetic kin. For example, S-trityl-l-cysteine (STC) and monastrol are HsEg5 inhibitors that bind to a su...

A sensitised RNAi screen reveals a ch-TOG genetic interaction network required for spindle assembly.

Sci. Rep. 5 , 10564, (2015)

How multiple spindle assembly pathways are integrated to drive bipolar spindle assembly is poorly understood. We performed an image-based double RNAi screen to identify genes encoding Microtubule-Asso...

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