Monastrol(Synonyms: (±)-Monastrol)

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Monastrol (Synonyms: (±)-Monastrol) 纯度: 99.70%

Monastrol是具有高效性和细胞渗透性的有丝分裂驱动蛋白 Eg5 的抑制剂,IC50 值为 14 μM。

Monastrol(Synonyms: (±)-Monastrol)

Monastrol Chemical Structure

CAS No. : 329689-23-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1608 In-stock
1 mg ¥500 In-stock
5 mg ¥800 In-stock
10 mg ¥1100 In-stock
25 mg ¥2300 In-stock
50 mg ¥3900 In-stock
100 mg ¥7000 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.

IC50 & Target

Eg5

14 μM (IC50)

体外研究
(In Vitro)

Monastrol is a small, cell-permeable molecule that arrests cells in mitosis by specifically inhibiting Eg5, a member of the Kinesin-5 family. Monastrol treatment of dividing cells results in spindle collapse and cell cycle arrest with a monoastral spindle, which is similar to the phenotype observed when Eg5 is inhibited by anti-Eg5 antibodies[1]. Monastrol is an allosteric inhibitor of the mitotic kinesin Eg5 that exhibits an antiproliferative effect against several cell lines. Monastrol treatment can decrease cell viability in MCF-7 tumor cells. Real-time cell growth kinetic analysis showed a decrease in the proliferation of MCF-7 cells exposed to monastrol[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

292.35

Formula

C14H16N2O3S

CAS 号

329689-23-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 33 mg/mL (112.88 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4206 mL 17.1028 mL 34.2056 mL
5 mM 0.6841 mL 3.4206 mL 6.8411 mL
10 mM 0.3421 mL 1.7103 mL 3.4206 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.55 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.55 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.55 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Cochran JC, et al. Monastrol inhibition of the mitotic kinesin Eg5. J BiolChem. 2005 Apr 1;280(13):12658-67.

    [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.

    [3]. 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.

Cell Assay
[2]

The cytotoxicity assay is performed with MTT. Cells are seeded in 96-well culture plates (5000 cells/well) and incubated for 24 h for stabilization. After this period, the following treatments are administered for 24 and 48 h: vehicle control (0.5 % DMSO); 1 μM doxorubicin and monastrol at 5, 25, 50, 75, and 100 μM. After each time of treatment, the medium is withdrawn, serum-free media containing 0.5 mg/mL MTT salt is added and incubated for 4 h, and formazan crystal products are diluted[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Cochran JC, et al. Monastrol inhibition of the mitotic kinesin Eg5. J BiolChem. 2005 Apr 1;280(13):12658-67.

    [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.

    [3]. 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.

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