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Monastrol {[allProObj[0].p_purity_real_show]}

货号：A101991 同义名： (±)-Monastrol

Monastrol是一种特异性且别构的有丝分裂分子马达Eg5抑制剂，IC50值为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 细胞实验

Cell Line
Concentration Treated Time Description References
RPE-1 cells 15 μM 40 min Reduced the frequency of lagging chromosomes Curr Biol. 2012 Feb 7;22(3):225-30.
CaCo-2 cells 15 μM 16 h Reduced the frequency of lagging chromosomes and spindle length Curr Biol. 2012 Feb 7;22(3):225-30.
HEK293T cells 25µM and 100µM 4 h and 24 h Monastrol treatment resulted in a pronounced increase in Mcl-1S mRNA content, but no increase at the protein level. 25µM Monastrol only slightly increased the proportion of cells in G2/M phase, while 100µM Monastrol effectively arrested cells in G2/M phase. Front Cell Dev Biol. 2020 Sep 25;8:543066.
Human induced pluripotent stem cells-derived secondary motor neurons 100 µmol and 10 µmol 48 h To evaluate the effect of Monastrol on the neurite outgrowth of secondary motor neurons, the results showed that Monastrol significantly and dose-dependently accelerated neurite outgrowth. J Neuroinflammation. 2023 Jun 9;20(1):139.
NOZ cells 15μM and 20μM 48 h Monastrol induced G2M phase cell cycle arrest and inhibited cell proliferation. Int J Biol Sci. 2021 Jan 1;17(2):514-526.
EH-GB1 cells 15μM and 20μM 48 h Monastrol induced G2M phase cell cycle arrest and inhibited cell proliferation. Int J Biol Sci. 2021 Jan 1;17(2):514-526.
U2OS cells 100μM 1 h or 6 h To investigate the effect of Monastrol treatment on cyclin A levels and k-MT attachment stability. Results showed that after 6 h of treatment, cyclin A levels decreased by 60%, and k-MT attachment stability significantly increased. Nature. 2013 Oct 3;502(7469):110-3.
Ptk2 cells 50 µM 4 h To test the effect of Monastrol on centrosome separation, it was found that Monastrol does not inhibit centrosome duplication but inhibits centrosome separation. J Cell Biol. 2000 Sep 4;150(5):975-88.
Xenopus egg extracts 50 µM To test the effect of Monastrol on bipolar spindle formation in Xenopus egg extracts, it was found that Monastrol inhibits the formation of bipolar spindles. J Cell Biol. 2000 Sep 4;150(5):975-88.
BS-C-1 cells 100 µM 4 h To test the effect of Monastrol on the cell cycle, it was found that Monastrol does not inhibit S phase, G2 phase, or mitotic entry, and the mitotic arrest it induces is reversible. J Cell Biol. 2000 Sep 4;150(5):975-88.

Monastrol 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Lewis rats Experimental autoimmune neuritis (EAN) model Intraperitoneal injection 1 mg/kg Injected on day 18, day 22, and day 26 To evaluate the effect of Monastrol on functional and histological recovery in the EAN model, the results showed that Monastrol significantly enhanced functional and histological recovery and accelerated the recovery of motor nerve conduction velocity. J Neuroinflammation. 2023 Jun 9;20(1):139.

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 292.35
SMILES Code O=C(C1=C(C)NC(NC1C2=CC=CC(O)=C2)=S)OCC
MDL No. MFCD00813077
别名 (±)-Monastrol
运输蓝冰
InChI Key LOBCDGHHHHGHFA-UHFFFAOYSA-N
Pubchem ID 2987927
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三

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 动物研究 | Monastrol 参考文献 | Monastrol 实验方案 | Monastrol 技术信息

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