Home Cytoskeletal Signaling Kinesin inhibitor Monastrol For research use only.

Monastrol

Synonyms: (±)-Monastrol

Monastrol ((±)-Monastrol) is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) with an IC50 of 14μM, which is essential for maintaining separation of the half-spindles.

Monastrol Chemical Structure

Monastrol Chemical Structure

CAS No. 329689-23-8

Purity & Quality Control

Monastrol Related Products

Signaling Pathway

Kinesin Signaling Pathways

Kinesin Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa Function assay 12 hrs Inhibition of Eg5 ATPase activity expressed in HeLa cells after 12 hrs, IC50=6.1μM 17587586
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
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
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 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay, EC50=24.155μM 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
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
HL-60(TB) Growth inhibition assay Growth inhibition of human HL-60(TB) cells, GI50=25.1μM 21855351
M14 Growth inhibition assay Growth inhibition of human M14 cells, GI50=25.1μM 21855351
CCRF-CEM Growth inhibition assay Growth inhibition of human CCRF-CEM cells, GI50=31.6μM 21855351
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
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
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
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
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
Click to View More Cell Line Experimental Data

Biological Activity

Description Monastrol ((±)-Monastrol) is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) with an IC50 of 14μM, which is essential for maintaining separation of the half-spindles.
Targets
KIF11(Eg5) [4]
(Cell-based assay)
14 μM
In vitro
In vitro

Monastrol does not inhibit progression through S and G2 phases of the cell cycle or centrosome duplication. The mitotic arrest due to monastrol is also rapidly reversible. Monastrol also inhibits bipolar spindle formation in Xenopus egg extracts. Monastrol arrests cells in mitosis with monoastral spindles comprised of a radial array of microtubules surrounded by a ring of chromosomes while it does not affect microtubules in interphase cells or microtubule polymerization in vitro[1]. Exposure of cultured sympathetic neurons to monastrol for a few hours increases both the number and the growth rate of the axons. With additional time, the overall lengths of the axons are indistinguishable from controls. Sensory neurons shows a similar short-term increase in axonal growth rate. However, prolonged exposure results in shorter axons, suggesting that sensory neurons may be more sensitive to toxic effects of the drug. Nevertheless, the overall health of the cultures is still far more robust than cultures treated with taxol, a drug commonly used for anti-cancer therapy[2]. In HeLa cells, monastrol activates the spindle checkpoint, leading to mitotic arrest and apoptosis[3].
Cell Research Cell lines BS-C-1 (monkey epithelial kidney) cells
Concentrations 100 μM
Incubation Time 4 h
Method

For the double thymidine arrest, exponentially growing BS-C-1 cells are cultured for 16 h in normal growth medium containing 2 mM thymidine. After this, the cells are released into normal growth medium supplemented with 24 μM deoxycytidine for 9 h. The second thymidine block is imposed for 16 h during which the cells were maintained in serum-free medium containing 2 mM thymidine. Finally, the cells are released into normal growth medium containing 24 μM deoxycytidine to which is added either 100 μM monastrol or 0.1% DMSO. To assess the reversibility of the effect of monastrol and nocodazole treatment, BS-C-1 cells plated on coverslips are treated for 4 h in normal growth medium containing either 2 μM nocodazole or 100 μM monastrol and then released into normal medium. At the different time points, coverslips are processed for immunofluorescence and the cells in interphase or mitosis are counted and categorized.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 26035434
Western blot Cyclin B / Survivin 26035434

Chemical Information & Solubility

Molecular Weight 292.35 Formula

C14H16N2O3S
CAS No. 329689-23-8 SDF Download Monastrol SDF
Smiles CCOC(=O)C1=C(NC(=S)NC1C2=CC(=CC=C2)O)C
Storage (From the date of receipt) 3 years -20°C(in the dark) powder

In vitro
Batch:

DMSO : 58 mg/mL ( (198.39 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 58 mg/mL

Water : Insoluble


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