Monastrol is a specific and allosteric inhibitor of mitotic molecular motor kinesin Eg5 with IC50 value of 14 μM.
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产品名称 | Kinesin ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SB-743921 HCl |
++++
KSP, Ki: 0.07 nM KSP (P388 cells), IC50: 14.4 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。 |
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 | ||
Dose | Hamster: 2.5 mg/kg - 20 mg/kg[3] (p.o.) |
Administration | p.o. |
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 |
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 |