|4-(3-羟基苯基)-6-甲基-2-硫代-1,2,3,4-四氢嘧啶-5-羧酸乙酯|CsnPharm

CAS No.: 329689-23-8

Monastrol Catalog No. CSN18931

Synonyms: (±)-Monastrol

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

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生物活性

实验方案

技术信息

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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动物研究
剂量
Hamster: 2.5 mg/kg - 20 mg/kg^[3] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Hamster: 2.5 mg/kg - 20 mg/kg^[3] (p.o.)
给药途径	p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4205 mL
- 17.1026 mL
- 34.2052 mL
- 5 mM
- 0.6841 mL
- 3.4205 mL
- 6.8410 mL
- 10 mM
- 0.3421 mL
- 1.7103 mL
- 3.4205 mL

技术信息

CAS号

329689-23-8

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H16N2O3S

运输

蓝冰

分子量

292.35

别名

(±)-Monastrol

溶解度

DMSO	58.0 mg/mL (198.4 mM)
Water	Insoluble
Ethanol	57.0 mg/mL (195.0 mM)

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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
HeLa cells	-	Function assay	12 h	Inhibition of Eg5 ATPase activity expressed in HeLa cells after 12 hrs, IC50=6.1 μM	17587586
HL-60(TB) cells	-	Growth inhibition assay	-	Growth inhibition of human HL-60(TB) cells, GI50=25.1 μM	21855351
hTERT-HME1 cells	-	Proliferation assay	72 h	Antiproliferative activity against human hTERT-HME1 cells after 72 hrs by Alamar blue assay, EC50=45.082 μM	20597485
K562 cells	-	Growth inhibition assay	-	Growth inhibition of human K562 cells, GI50=31.6 μM	21855351
KBV1 cells	-	Proliferation assay	72 h	Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay in presence of zosuquidar, EC50=45.394 μM	20597485
KM12 cells	-	Growth inhibition assay	-	Growth inhibition of human KM12 cells, GI50=31.6 μM	21855351
M14 cells	-	Growth inhibition assay	-	Growth inhibition of human M14 cells, GI50=25.1 μM	21855351
MOLT4 cells	-	Growth inhibition assay	-	Growth inhibition of human MOLT4 cells, GI50=31.6 μM	21855351
NCI-H322M cells	-	Growth inhibition assay	-	Growth inhibition of human NCI-H322M cells, GI50=39.8 μM	21855351
NCI-H522 cells	-	Growth inhibition assay	-	Growth inhibition of human NCI-H522 cells, GI50=31.6 μM	21855351
SF295 cells	-	Growth inhibition assay	-	Growth inhibition of human SF295 cells, GI50=31.6 μM	21855351
SK-MEL-5 cells	-	Growth inhibition assay	-	Growth inhibition of human SK-MEL-5 cells, GI50=39.8 μM	21855351
SR cells	-	Growth inhibition assay	-	Growth inhibition of human SR cells, GI50=31.6 μM	21855351
SW620 cells	-	Growth inhibition assay	-	Growth inhibition of human SW620 cells, GI50=39.8 μM	21855351
UACC62 cells	-	Growth inhibition assay	-	Growth inhibition of human UACC62 cells, GI50=39.8 μM	21855351

Monastrol Catalog No. CSN18931

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