Monastrol (Synonyms: (±)-Monastrol) |
Catalog No.GC14929
One-Click Copy Product Info
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Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 254753-54-3;329689-23-8
Sample solution is provided at 25 µL, 10mM.
Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14μM[1]. Eg5 is a homotetrameric motor protein of the kinesin-5 family that uses ATP hydrolysis to slide along microtubules, playing a central role in spindle-pole separation and maintaining the bipolarity of the mitotic spindle[2]. Monastrol, by binding the allosteric pocket of Eg5, blocks ADP release and suppresses the motor’s microtubule-based motility, serving as a widely employed tool for dissecting cell division, spindle dynamics, and anti-cancer mechanisms[3][4].
In vitro, Monastrol (5–100μM; 24–48h) selectively suppressed MCF-7 breast-cancer cell proliferation, reduced cell viability, lowered the normalized cell index by 30–40%, arrested cells in G1 and G2/M, raised the mitotic index and up-regulated p21/CDKN1A mRNA, all without inducing apoptosis[5]. Monastrol (100µM; 48h) significantly inhibited the invasion ability of HCT-116 and DLD-1 colorectal cancer cells with high fascin expression[6].
In vivo, Monastrol (1mg/kg; i.p.; twice weekly for 4 weeks; given 10min before each bortezomib dose) reversed bortezomib-induced sensory neuropathy in C57BL/6 mice, shortening tail sensory latency by 25% and cold-withdrawal time by 40%, fully preserving intra-epidermal nerve fiber density, and restoring sciatic/tibial unmyelinated fiber caliber while attenuating axonal atrophy[7].
References:
[1] Mayer TU, Kapoor TM, Haggarty SJ, King RW, Schreiber SL, Mitchison TJ. Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen. Science. 1999;286(5441):971-974.
[2] Mann BJ, Wadsworth P. Kinesin-5 Regulation and Function in Mitosis. Trends Cell Biol. 2019;29(1):66-79.
[3] Maliga Z, Mitchison TJ. Small-molecule and mutational analysis of allosteric Eg5 inhibition by monastrol. BMC Chem Biol. 2006;6:2.
[4] Garcia-Saez I, Skoufias DA. Eg5 targeting agents: From new anti-mitotic based inhibitor discovery to cancer therapy and resistance. Biochem Pharmacol. 2021;184:114364.
[5] Marques LA, Semprebon SC, Niwa AM, et al. Antiproliferative activity of monastrol in human adenocarcinoma (MCF-7) and non-tumor (HB4a) breast cells. Naunyn Schmiedebergs Arch Pharmacol. 2016;389(12):1279-1288.
[6] Alburquerque-González B, Montoro-García S, Bernabé-García Á, et al. Monastrol suppresses invasion and metastasis in human colorectal cancer cells by targeting fascin independent of kinesin-Eg5 pathway. Biomed Pharmacother. 2024;175:116785.
[7] Bobylev I, Peters D, Vyas M, et al. Kinesin-5 Blocker Monastrol Protects Against Bortezomib-Induced Peripheral Neurotoxicity. Neurotox Res. 2017;32(4):555-562.
| Cell experiment [1]: | |
Cell lines | human breast adenocarcinoma MCF-7 cells |
Preparation Method | The human breast adenocarcinoma MCF-7 cells were grown in DMEM supplemented with 10% fetal bovine serum (FBS) and 1% penicillin/streptomycin at 37°C and 5% CO2. Monastrol was dissolved in dimethyl sulfoxide (DMSO) and diluted in Dulbecco’s modified Eagle’s medium, where the concentration of DMSO did not exceed 0.5% in culture. The cytotoxicity assay was performed with MTT assay. Cells were seeded in 96-well culture plates (5×103 cells/well) and incubated for 24h for stabilization. After this period, the following treatments were administered for 24 and 48h: vehicle control (0.5% DMSO) and Monastrol at 5, 25, 50, 75, and 100μM. After each time of treatment, the medium was withdrawn, serum-free media containing 0.5mg/mL MTT salt was added and incubated for 4h, and formazan crystal products were diluted. The absorbance at 540nm was converted to a percentage of surviving cells. The assay was performed in triplicate in three independent experiments. The xCELLigence–real-time cell analyzer (RTCA) system was used to monitor the dynamics of cell proliferation using the electric impedance. |
Reaction Conditions | 5–100μM; 24–48h |
Applications | Monastrol selectively suppressed MCF-7 breast-cancer cell proliferation, reduced cell viability. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Adult wild-type C57BL/6J mice were housed under standard conditions with regulated temperature (21 ± 1°C), under reversed 12/12h (light/dark) cycle, with food and water ad libitum. Bortezomib was dissolved in 100% dehydrated ethanol (1.2mg/ml) and diluted 1:1 with 0.9% saline. Monastrol was dissolved in DMSO (10mg/ml) and diluted 1:10 with 0.9% saline. Mice (N = 5 per group) were treated with either 0.6mg/kg BZ intravenously (i.v.) or with a combination of 1mg/kg Monastrol intraperitoneally (i.p.), 10min prior to 0.6mg/kg BZ treatment. The control group (CTRL) was treated with vehicle i.v. (100% dehydrated ethanol and 0.9% saline, diluted 1:1). All groups were treated twice per week for 4 weeks. For the measurement of the sensory nerve conduction, the needle electrodes were placed on the tail. The measurements were performed 20min before the first administration of the drugs (day 0) and 24h after the last administration (day 28). |
Dosage form | 1mg/kg; i.p.; twice weekly for 4 weeks; given 10min before each bortezomib dose |
Applications | Monastrol reversed bortezomib-induced sensory neuropathy in C57BL/6 mice, shortening tail sensory latency by 25%. |
References: | |
| Cas No. | 254753-54-3;329689-23-8 | SDF | |
| Synonyms | (±)-Monastrol | ||
| Chemical Name | ethyl 6-(3-hydroxyphenyl)-2-mercapto-4-methyl-1,6-dihydropyrimidine-5-carboxylate | ||
| Canonical SMILES | CCOC(C(C1C2=CC(O)=CC=C2)=C(N=C(S)N1)C)=O | ||
| Formula | C14H16N2O3S | M.Wt | 292.35 |
| Solubility | ≥ 29.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4206 mL | 17.1028 mL | 34.2056 mL |
| 5 mM | 684.1 μL | 3.4206 mL | 6.8411 mL |
| 10 mM | 342.1 μL | 1.7103 mL | 3.4206 mL |
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)