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Monastrol Kinesin inhibitor

Name: Monastrol
Brand: Selleck Chemicals
SKU: S8439
Rating: 5 (19 reviews)

Cat.No.S8439

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.

Chemical Structure

Molecular Weight: 292.35

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Quality Control

Batch: Purity: 99.86%

99.86

Related Targets	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Other Kinesin Inhibitors	GSK923295 Ispinesib (SB-715992) SB743921 HCl ARQ 621 K 858 BTB-1 VLS-1488(KIF18A-IN-6 ) H-Cys(Trt)-OH Filanesib hydrochloride GW406108X

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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

Chemical Information, Storage & Stability

Molecular Weight	292.35	Formula	C₁₄H₁₆N₂O₃S	Storage (From the date of receipt)	3 years -20°C(in the dark) powder
CAS No.	329689-23-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	(±)-Monastrol			Smiles	CCOC(=O)C1=C(NC(=S)NC1C2=CC(=CC=C2)O)C

Solubility

In vitro
Batch:

DMSO : 58 mg/mL (198.39 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 58 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.900mg/ml (9.92mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.710mg/ml (2.43mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	KIF11(Eg5) (Cell-based assay) 14 μM
In vitro	Monastrol does not inhibit progression through S and G2 phases of the cell cycle or centrosome duplication. The mitotic arrest due to this compound is also rapidly reversible. It also inhibits bipolar spindle formation in Xenopus egg extracts. This chemical 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. Exposure of cultured sympathetic neurons to this compound 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 show 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. In HeLa cells, this compound activates the spindle checkpoint, leading to mitotic arrest and apoptosis.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10973989/ [2] https://pubmed.ncbi.nlm.nih.gov/14983520/ [3] https://pubmed.ncbi.nlm.nih.gov/17041103/ [4] https://pubmed.ncbi.nlm.nih.gov/10542155/

Applications

Methods	Biomarkers	Images	PMID
Growth inhibition assay	Cell viability		26035434
Western blot	Cyclin B / Survivin		26035434

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