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Monastrol

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Chemical Structure| 329689-23-8 同义名 : (±)-Monastrol
CAS号 : 329689-23-8
货号 : A101991
分子式 : C14H16N2O3S
纯度 : 98%
分子量 : 292.353
MDL号 : MFCD00813077
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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
实验方案
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
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.