Monastrol
别名: (±)-Monastrol
此产品请避光密封保存。
Monastrol ((±)-Monastrol)是一种具有细胞透性的kinesin-5(KIF11)小分子抑制剂，IC50为14μM，kinesin-5(KIF11)可保持半纺锤体的分离状态。
Monastrol Chemical Structure
CAS: 329689-23-8
产品质控
批次：
纯度：
99.86%
99.86
Monastrol相关产品
| 相关靶点 | Kinesin-12 | 点击展开 |
|---|---|---|
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| 相关化合物库 | 激酶抑制剂库 血管生成相关化合物库 TGF-beta/Smad信号通路库 细胞骨架信号通路化合物库 抗心血管疾病化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| C6 | Antiproliferative assay | 100 uM | 24 hrs | Antiproliferative activity against rat C6 cells assessed as reduction in cell viability at 100 uM after 24 hrs by MTS assay relative to control | ChEMBL |
| C6 | Cell cycle assay | 100 uM | 24 hrs | Cell cycle arrest in rat C6 cells assessed as accumulation at G2/M phase at 100 uM after 24 hrs by propidium iodide staining based flow cytometry | ChEMBL |
| U138MG | Apoptosis assay | 200 uM | 48 hrs | Induction of apoptosis in human U138MG cells at 200 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry | ChEMBL |
| U138MG | Necrosis assay | 200 uM | 48 hrs | Induction of necrosis in human U138MG cells at 200 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry | ChEMBL |
| C6 | Apoptosis assay | 100 uM | 48 hrs | Induction of apoptosis in rat C6 cells at 100 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry | ChEMBL |
| U138MG | Function assay | 200 uM | 24 hrs | Inhibition of EG5 in human U138MG cells assessed as monopolar spindle formation at 200 uM after 24 hrs by Hoechst staining based immunofluorescence microscopic method | ChEMBL |
| C6 | Function assay | 100 uM | 24 hrs | Inhibition of EG5 in rat C6 cells assessed as monopolar spindle formation at 100 uM after 24 hrs by Hoechst staining based immunofluorescence microscopic method | ChEMBL |
| C6 | Antiproliferative assay | 5 to 50 uM | 48 hrs | Antiproliferative activity against rat C6 cells at 5 to 50 uM after 48 hrs by Neubauer chamber method | ChEMBL |
| MCF7 | Antiproliferative assay | 25 uM | 48 hrs | Antiproliferative activity against human MCF7 cells at 25 uM after 48 hrs by sulforhodamine B assay | ChEMBL |
| NCI/ADR-RES | Antiproliferative assay | 25 uM | 48 hrs | Antiproliferative activity against human NCI/ADR-RES cells at 25 uM after 48 hrs by sulforhodamine B assay | ChEMBL |
| 786-0 | Antiproliferative assay | 25 uM | 48 hrs | Antiproliferative activity against human 786-0 cells at 25 uM after 48 hrs by sulforhodamine B assay | ChEMBL |
| HT-29 | Antiproliferative assay | 25 uM | 48 hrs | Antiproliferative activity against human HT-29 cells at 25 uM after 48 hrs by sulforhodamine B assay | ChEMBL |
| UACC62 | Antiproliferative assay | 25 uM | 48 hrs | Antiproliferative activity against human UACC62 cells at 25 uM after 48 hrs by sulforhodamine B assay | ChEMBL |
| PC3 | Antiproliferative assay | 25 uM | 48 hrs | Antiproliferative activity against human PC3 cells at 25 uM after 48 hrs by sulforhodamine B assay | ChEMBL |
| OVCAR3 | Antiproliferative assay | 25 uM | 48 hrs | Antiproliferative activity against human OVCAR3 cells at 25 uM after 48 hrs by sulforhodamine B assay | ChEMBL |
| KBV1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay in presence of zosuquidar, EC50=45.394μM | 20597485 | |
| hTERT-HME1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human hTERT-HME1 cells after 72 hrs by Alamar blue assay, EC50=45.082μM | 20597485 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay, EC50=24.155μM | 20597485 | |
| HeLa | Function assay | 12 hrs | Inhibition of Eg5 ATPase activity expressed in HeLa cells after 12 hrs, IC50=6.1μM | 17587586 | |
| HL-60(TB) | Growth inhibition assay | 24 hrs | Growth inhibition of human HL-60(TB) cells incubated for 24 hrs by MTT assay, IC50=0.147μM | 28667871 | |
| MOLT4 | Growth inhibition assay | 24 hrs | Growth inhibition of human MOLT4 cells incubated for 24 hrs by MTT assay, IC50=0.215μM | 28667871 | |
| McCoy | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse McCoy cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=26.8μM | 29908443 | |
| MM1S | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MM1S cells incubated for 72 hrs by MTT assay, IC50=8.7μM | ChEMBL | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay, IC50=9μM | ChEMBL | |
| CCRF-CEM | Growth inhibition assay | Growth inhibition of human CCRF-CEM cells, GI50=31.6μM | 21855351 | ||
| M14 | Growth inhibition assay | Growth inhibition of human M14 cells, GI50=25.1μM | 21855351 | ||
| HL-60(TB) | Growth inhibition assay | Growth inhibition of human HL-60(TB) cells, GI50=25.1μM | 21855351 | ||
| KBV1/KB3-1 | Function assay | Drug resistant ratio of EC50 for human KBV1 cells overexpressing MDR1 to EC50 for KB3-1 cells, EC50=0.0012μM | 20597485 | ||
| HCT116 | Cell cycle assay | Effect on cell cycle progression in human HCT116 cells assessed as increase in phospho-histone H3 by fluorescence microscopy, EC50=1.5μM | 18793847 | ||
| HCT116 | Cell cycle assay | Effect on cell cycle progression in human HCT116 cells assessed as mitotic arrest measured by doubling DNA content by fluorescence microscopy, EC50=1.2μM | 18793847 | ||
| K562 | Growth inhibition assay | Growth inhibition of human K562 cells, GI50=31.6μM | 21855351 | ||
| MOLT4 | Growth inhibition assay | Growth inhibition of human MOLT4 cells, GI50=31.6μM | 21855351 | ||
| SR | Growth inhibition assay | Growth inhibition of human SR cells, GI50=31.6μM | 21855351 | ||
| NCI-H522 | Growth inhibition assay | Growth inhibition of human NCI-H522 cells, GI50=31.6μM | 21855351 | ||
| COLO205 | Growth inhibition assay | Growth inhibition of human COLO205 cells, GI50=31.6μM | 21855351 | ||
| HCT116 | Growth inhibition assay | Growth inhibition of human HCT116 cells, GI50=31.6μM | 21855351 | ||
| KM12 | Growth inhibition assay | Growth inhibition of human KM12 cells, GI50=31.6μM | 21855351 | ||
| SF295 | Growth inhibition assay | Growth inhibition of human SF295 cells, GI50=31.6μM | 21855351 | ||
| U251 | Growth inhibition assay | Growth inhibition of human U251 cells, GI50=31.6μM | 21855351 | ||
| SK-MEL-2 | Growth inhibition assay | Growth inhibition of human SK-MEL-2 cells, GI50=31.6μM | 21855351 | ||
| RPMI8266 | Growth inhibition assay | Growth inhibition of human RPMI8266 cells, GI50=31.6μM | 21855351 | ||
| NCI-H322M | Growth inhibition assay | Growth inhibition of human NCI-H322M cells, GI50=39.8μM | 21855351 | ||
| HCC2998 | Growth inhibition assay | Growth inhibition of human HCC2998 cells, GI50=39.8μM | 21855351 | ||
| HCT15 | Growth inhibition assay | Growth inhibition of human HCT15 cells, GI50=39.8μM | 21855351 | ||
| SW620 | Growth inhibition assay | Growth inhibition of human SW620 cells, GI50=39.8μM | 21855351 | ||
| SNB75 | Growth inhibition assay | Growth inhibition of human SNB75 cells, GI50=39.8μM | 21855351 | ||
| SK-MEL-5 | Growth inhibition assay | Growth inhibition of human SK-MEL-5 cells, GI50=39.8μM | 21855351 | ||
| UACC62 | Growth inhibition assay | Growth inhibition of human UACC62 cells, GI50=39.8μM | 21855351 | ||
| SN12C | Growth inhibition assay | Growth inhibition of human SN12C cells, GI50=39.8μM | 21855351 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Monastrol ((±)-Monastrol)是一种具有细胞透性的kinesin-5(KIF11)小分子抑制剂，IC50为14μM，kinesin-5(KIF11)可保持半纺锤体的分离状态。 | ||
|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Monastrol并不是通过细胞周期的S期和G2期或中心体复制抑制细胞周期进程。monastrol的有丝分裂阻滞作用快速可逆。它还能在爪蟾卵提取物中抑制双极纺锤体的形成。Monastrol将细胞阻滞在有丝分裂期，但在体外不影响处于有丝分裂间期细胞的微管或是微管聚合[1]。将交感神经元细胞暴露于monastrol几小时，将会增加轴突数量及生长速率。但时间延长，轴突的总体长度则与对照组无异。感觉神经元同样也有这种轴突生长速率短期升高的效果，然而，进一步延长暴露时间将导致轴突变短，说明感觉神经元细胞对药物的毒性作用更为敏感。但是，细胞整体培养状况比taxol处理组要更为强健，taxol是一种常用于治疗癌症的药物[2]。在HeLa细胞中，monastrol激活纺锤体检验点，导致有丝分裂受到阻滞，引起凋亡[3]。 |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | BS-C-1 (猴肾脏上皮)细胞 | ||
| 浓度 | 100 μM | |||
| 孵育时间 | 4 h | |||
| 方法 | 在胸腺嘧啶脱氧核苷双重阻滞实验中，处于生长对数期的BS-C-1细胞在含2 mM胸苷的正常培养基中培养。然后将细胞置于含24 μM deoxycytidine的培养基中培养9小时。第二次阻滞时，将细胞至于要含2 mM 胸苷的无血清培养基中16小时。最后，将细胞重新置于含24 μM deoxycytidine的培养基中，加入100 μM monastrol或0.1% DMSO。为了检测monastrol和nocodazole的作用是否具有可逆性。将BS-C-1铺于盖玻片上，用含2 μM nocodazole或是100 μM monastrol的正常生长培养基处理4小时，然后将细胞置于正常培养基。在不同的时间节点，将盖玻片进行免疫荧光染色，对处于有丝分裂间期或有丝分裂期的细胞进行计数。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Growth inhibition assay | Cell viability |
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26035434 | |
| Western blot | Cyclin B / Survivin |
|
26035434 | |
化学信息&溶解度
| 分子量 | 292.35 | 分子式 | C14H16N2O3S |
| CAS号 | 329689-23-8 | SDF | Download Monastrol SDF |
| Smiles | CCOC(=O)C1=C(NC(=S)NC1C2=CC(=CC=C2)O)C | ||
| 储存条件(自收到货起) | 3年 -20°C(避光) 粉状 | ||
|
体外溶解度 |
DMSO : 58 mg/mL ( (198.39 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 58 mg/mL (198.39 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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