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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Monastrol
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
329689-23-8
- 规格：
50mg/1mg/5mg/10mg/25mg
| 规格： | 50mg | 产品价格： | ￥3190.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥310.0 |
| 规格： | 5mg | 产品价格： | ￥790.0 |
| 规格： | 10mg | 产品价格： | ￥1090.0 |
| 规格： | 25mg | 产品价格： | ￥1990.0 |
Monastrol是一种具有细胞透性的kinesin-5(KIF11)小分子抑制剂。
| 基本信息 | |
| CAS | No.329689-23-8 |
| 英文名称 | Monastrol |
| 别名 | (±)-Monastrol |
| 分子式 | C14H16N2O3S |
| 分子量 | 292.35 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC | EINECS 200-258-5 |
| MDL | MFCD00813077 |
| SMILES | O=C(C1=C(C)NC(NC1C2=CC=CC(O)=C2)=S)OCC |
| InChIKey | LOBCDGHHHHGHFA-UHFFFAOYSA-N |
| InChI | InChI=1S/C14H16N2O3S/c1-3-19-13(18)11-8(2)15-14(20)16-12(11)9-5-4-6-10(17)7-9/h4-7,12,17H,3H2,1-2H3,(H2,15,16,20) |
| PubChem CID | 2987927 |
| 靶点 | Kinesin |
| 通路 | Cytoskeleton |
| 背景说明 | Monastrol是一种具有细胞透性的kinesin-5(KIF11)小分子抑制剂。 |
| 生物活性 | Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.[1-3] |
| IC50 | IC50：14 μM（Eg5）[1-3] |
| In Vitro | We have used steady-state and presteady-state kinetics as well as equilibrium binding approaches to define the mechanistic basis of S-monastrol inhibition of monomeric human Eg5/KSP. In the absence of microtubules (Mts)， the basal ATPase activity is inhibited through slowed product release. In the presence of microtubules， the ATPase activity is also reduced with weakened binding of Eg5 to microtubules during steady-state ATP turnover. Monastrol-treated Eg5 also shows a decreased relative affinity for microtubules under equilibrium conditions. The Mt.Eg5 presteady-state kinetics of ATP binding and the subsequent ATP-dependent isomerization are unaffected during the first ATP turnover. However， monastrol appears to stabilize a conformation that allows for reversals at the ATP hydrolysis step. Monastrol promotes a dramatic decrease in the observed rate of Eg5 association with microtubules， and ADP release is slowed without trapping the Mt.Eg5.ADP intermediate.[1] |
| 细胞实验 | 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]. |
| 数据来源文献 | [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. |
| 单位 | 支 |
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IM1040 Monastrol 细胞骨架 索莱宝
￥310 - 3190
