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Monastrol

別名: (±)-Monastrol

此產(chǎn)品請避光密封保存。

Monastrol ((±)-Monastrol)是一種具有細(xì)胞透性的kinesin-5(KIF11)小分子抑制劑，IC50為14μM，kinesin-5(KIF11)可保持半紡錘體的分離狀態(tài)。

Monastrol Chemical Structure

Monastrol Chemical Structure

CAS: 329689-23-8

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mg 1204.01 現(xiàn)貨
50mg 4070.85 現(xiàn)貨
200mg 12039.31 現(xiàn)貨
1g 32678.74 現(xiàn)貨
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Monastrol相關(guān)產(chǎn)品

相關(guān)信號通路圖

Kinesin Signaling Pathways

Kinesin信號通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Monastrol ((±)-Monastrol)是一種具有細(xì)胞透性的kinesin-5(KIF11)小分子抑制劑，IC50為14μM，kinesin-5(KIF11)可保持半紡錘體的分離狀態(tài)。
靶點(diǎn)
KIF11(Eg5) [4]
(Cell-based assay)
14 μM
體外研究(In Vitro)
體外研究活性

Monastrol并不是通過細(xì)胞周期的S期和G2期或中心體復(fù)制抑制細(xì)胞周期進(jìn)程。monastrol的有絲分裂阻滯作用快速可逆。它還能在爪蟾卵提取物中抑制雙極紡錘體的形成。Monastrol將細(xì)胞阻滯在有絲分裂期，但在體外不影響處于有絲分裂間期細(xì)胞的微管或是微管聚合[1]。將交感神經(jīng)元細(xì)胞暴露于monastrol幾小時(shí)，將會(huì)增加軸突數(shù)量及生長速率。但時(shí)間延長，軸突的總體長度則與對照組無異。感覺神經(jīng)元同樣也有這種軸突生長速率短期升高的效果，然而，進(jìn)一步延長暴露時(shí)間將導(dǎo)致軸突變短，說明感覺神經(jīng)元細(xì)胞對藥物的毒性作用更為敏感。但是，細(xì)胞整體培養(yǎng)狀況比taxol處理組要更為強(qiáng)健，taxol是一種常用于治療癌癥的藥物[2]。在HeLa細(xì)胞中，monastrol激活紡錘體檢驗(yàn)點(diǎn)，導(dǎo)致有絲分裂受到阻滯，引起凋亡[3]。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 BS-C-1 (猴腎臟上皮)細(xì)胞
濃度 100 μM
孵育時(shí)間 4 h
方法

在胸腺嘧啶脫氧核苷雙重阻滯實(shí)驗(yàn)中，處于生長對數(shù)期的BS-C-1細(xì)胞在含2 mM胸苷的正常培養(yǎng)基中培養(yǎng)。然后將細(xì)胞置于含24 μM deoxycytidine的培養(yǎng)基中培養(yǎng)9小時(shí)。第二次阻滯時(shí)，將細(xì)胞至于要含2 mM 胸苷的無血清培養(yǎng)基中16小時(shí)。最后，將細(xì)胞重新置于含24 μM deoxycytidine的培養(yǎng)基中，加入100 μM monastrol或0.1% DMSO。為了檢測monastrol和nocodazole的作用是否具有可逆性。將BS-C-1鋪于蓋玻片上，用含2 μM nocodazole或是100 μM monastrol的正常生長培養(yǎng)基處理4小時(shí)，然后將細(xì)胞置于正常培養(yǎng)基。在不同的時(shí)間節(jié)點(diǎn)，將蓋玻片進(jìn)行免疫熒光染色，對處于有絲分裂間期或有絲分裂期的細(xì)胞進(jìn)行計(jì)數(shù)。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Growth inhibition assay Cell viability 26035434
Western blot Cyclin B / Survivin 26035434

化學(xué)信息&溶解度

分子量 292.35 分子式

C14H16N2O3S
CAS號 329689-23-8 SDF Download Monastrol SDF
Smiles CCOC(=O)C1=C(NC(=S)NC1C2=CC(=CC=C2)O)C
儲存條件(自收到貨起) 3年 -20°C(避光) 粉狀

體外溶解度
批次：

DMSO : 58 mg/mL ( (198.39 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO)

Ethanol : 58 mg/mL (198.39 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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