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Monastrol {[allProObj[0].p_purity_real_show]}

货号：A101991 同义名： (±)-Monastrol

Monastrol is a specific and allosteric inhibitor of mitotic molecular motor kinesin Eg5 with IC50 value of 14 μM.

Monastrol 化学结构 CAS号：329689-23-8
Monastrol 化学结构
CAS号：329689-23-8
Monastrol 3D分子结构
CAS号：329689-23-8
Monastrol 化学结构 CAS号：329689-23-8
Monastrol 3D分子结构 CAS号：329689-23-8
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Monastrol 纯度/质量文件 产品仅供科研

货号：A101991 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Kinesin ↓ 其他靶点 纯度
SB-743921 HCl ++++

KSP (P388 cells), IC50: 14.4 nM

KSP, Ki: 0.07 nM

 		99%+
GSK-923295 ++

CENP-E, Ki: 3.2 nM

 		99%+
Ispinesib +++

KSP (HsEg5), Ki app: 1.7 nM

 		99%+
AZ3146 +

Mps1, IC50: ~35 nM

 		98+%
MPI-0479605 ++

Mps1, IC50: 1.8 nM

 		99%+
BAY1217389 +++

Mps1, IC50: 0.63 nM

 		98%
ARQ 621 ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Monastrol 生物活性

描述 Kinesin-5 motors are one of the members of microtubule-dependent superfamily which are responsible for generating outward forces for establishing and maintaining spindle bipolarity and contributing to microtubule flux[3]. Monastrol is a cell-permeable inhibitor of the kinesin-5 with IC50 value of 9 - 22 µM for all kinesin-5 constructs[4]. The HeLa cells were treated with 100 μmol/L of monastrol for 30 hours. The mitotic index was determined using formaldehyde fix and Hoechst DNA stain and it was found that the treatment of monastrol induced mitotic arrest which peaked at 18 hours. The poly (ADP-ribose) polymerase coincided was cleavage and the mitotic marker phospho-histone H3 level was decreased after the treatment of monastrol as analyzed by western blotting assay[5]. The C57BL/6J mice were treated with 1 mg/kg monastrol intraperitoneally 10 min before the treatment of bortezomib for 28 days. The treatment of monastrol substantially alleviated morphological features of axonal injury and functional measures of sensory neuropathy as examined by H&E staining[6].
作用机制 The monastrol binds a complex of kinesin-5 and ADP. It inhibited the release of the microtubule-stimulated ADP from kinesin-5 through an allosteric mechanism[7].

Monastrol 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
CCRF-CEM cells Growth inhibition assay Growth inhibition of human CCRF-CEM cells, GI50=31.6 μM 21855351
HCC2998 cells Growth inhibition assay Growth inhibition of human HCC2998 cells, GI50=39.8 μM 21855351
HCT116 cells Function assay Effect on cell cycle progression in human HCT116 cells assessed as mitotic arrest measured by doubling DNA content by fluorescence microscopy, EC50=1.2 μM 18793847
HCT15 cells Growth inhibition assay Growth inhibition of human HCT15 cells, GI50=39.8 μM 21855351

Monastrol 动物研究

Dose Hamster: 2.5 mg/kg - 20 mg/kg[3] (p.o.)
Administration p.o.

Monastrol 参考文献

[1]Chin GM, Herbst R. Induction of apoptosis by monastrol, an inhibitor of the mitotic kinesin Eg5, is independent of the spindle checkpoint. Mol Cancer Ther. 2006 Oct;5(10):2580-91.

[2]Kapoor TM, Mayer TU, et al. Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5. J Cell Biol. 2000 Sep 4;150(5):975-88.

[3]Ferenz NP, Gable A, Wadsworth P. Mitotic functions of kinesin-5. Semin Cell Dev Biol. 2010 May;21(3):255-9.

[4]DeBonis S, Simorre JP, Crevel I, Lebeau L, Skoufias DA, Blangy A, Ebel C, Gans P, Cross R, Hackney DD, Wade RH, Kozielski F. Interaction of the mitotic inhibitor monastrol with human kinesin Eg5. Biochemistry. 2003 Jan 21;42(2):338-49.

[5]Chin GM, Herbst R. Induction of apoptosis by monastrol, an inhibitor of the mitotic kinesin Eg5, is independent of the spindle checkpoint. Mol Cancer Ther. 2006 Oct;5(10):2580-91.

[6]Bobylev I, Peters D, Vyas M, Barham M, Klein I, von Strandmann EP, Neiss WF, Lehmann HC. Kinesin-5 Blocker Monastrol Protects Against Bortezomib-Induced Peripheral Neurotoxicity. Neurotox Res. 2017 Nov;32(4):555-562.

[7]Maliga Z, Kapoor TM, Mitchison TJ. Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5. Chem Biol. 2002 Sep;9(9):989-96.

Monastrol 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.42mL

0.68mL

0.34mL

17.10mL

3.42mL

1.71mL

34.21mL

6.84mL

3.42mL

Monastrol 技术信息

CAS号329689-23-8
分子式C14H16N2O3S
分子量 292.353
别名 (±)-Monastrol
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C
溶解度

DMSO: 35 mg/mL(119.72 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Monastrol | 329689-23-8 | (±)-Monastrol | Kinesin | Mitotic Kinesin Eg5 Inhibitor | Cell Cycle/DNA Damage | Cytoskeleton | Apoptosis | Kinesin | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Monastrol 纯度/质量文件 | Monastrol 亚型比较 | Monastrol 生物活性 | Monastrol 细胞研究 | Monastrol 动物研究 | Monastrol 参考文献 | Monastrol 实验方案 | Monastrol 技术信息

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