Nocodazole (Synonyms: NSC 238159, Oncodazole, R 17934) |
| Catalog No.GC14075 |
Nocodazole is an anti-mitotic drug and a rapid and reversible microtubule polymerization inhibitor. It inhibits Abl, Abl (E255K), and Abl (T315I) in cell-free assays with IC50 values of 0.21μM, 0.53μM, and 0.64μM, respectively.
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Cas No.: 31430-18-9
Sample solution is provided at 25 µL, 10mM.
Nocodazole is an anti-mitotic drug and a rapid and reversible microtubule polymerization inhibitor. It inhibits Abl, Abl (E255K), and Abl (T315I) in cell-free assays with IC50 values of 0.21μM, 0.53μM, and 0.64μM, respectively[1]. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, thereby arresting mitosis and inducing apoptosis in tumor cells[2]. Nocodazole can increase CRISPR-mediated homologous recombination efficiency, enhancing the precision of gene editing efficacy[3].
In vitro, Nocodazole (50 ng/ml) treatment of HuH7 cells for 16 hours synchronizes approximately 50% of the cells at the G2/M phase, with intracellular microtubule fibers mainly distributed in the peripheral region of the cells and without forming a bipolar spindle[4]. Nocodazole (20µM) treatment of emsCOS-1 cells for 30 minutes results in the dispersion of Golgi stacks throughout the cytoplasm[5]. Nocodazole (1 nM) treatment of CHO cells inhibits microtubule dynamics, slowing migration and increasing the frequency and duration of the resting state while maintaining cell directionality. Nocodazole (70nM) has the opposite effect of low drug concentrations, causing cells to move more randomly[6].
In vivo, Nocodazole (5 mg/kg) administered intraperitoneally for six weeks significantly reduces the tumor volume and weight in mice transplanted with COLO 205 tumors, with enhanced antitumor effects observed when combined with ketoconazole[7].
References:
[1] Park H, Hong S. Nocodazole is a high-affinity ligand for the cancer-related kinases ABL, c-KIT, BRAF, and MEK[J]. ChemMedChem, 2011, 7(1): 53-56.
[2] Jordan M A, Wilson L. Microtubules and actin filaments: dynamic targets for cancer chemotherapy[J]. Current opinion in cell biology, 1998, 10(1): 123-130.
[3] Chen S, Chen D, Liu B, et al. Modulating CRISPR/Cas9 genome-editing activity by small molecules[J]. Drug Discovery Today, 2022, 27(4): 951-966.
[4] Makiyama T, Obama T, Watanabe Y, et al. Behavior of intracellular lipid droplets during cell division in HuH7 hepatoma cells[J]. Experimental Cell Research, 2023, 433(2): 113855.
[5] Mukai, K., Konno, H., Akiba, T. et al. Activation of STING requires palmitoylation at the Golgi[J]. Nat Commun 7, 11932 (2016).
[6] Ganguly A, Yang H, Sharma R, Patel KD, Cabral F. The role of microtubules and their dynamics in cell migration[J]. J Biol Chem. 2012, 287(52):43359-69.
[7] Wang Y J, Jeng J H, Chen R J, et al. Ketoconazole potentiates the antitumor effects of nocodazole: In vivo therapy for human tumor xenografts in nude mice[J]. Molecular Carcinogenesis: Published in cooperation with the University of Texas MD Anderson Cancer Center, 2002, 34(4): 199-210.
| Cell experiment [1]: | |
Cell lines | HuH7 cells |
Preparation Method | HuH7 cells were grown in Dulbecco's modified Eagle's medium supplemented with 10 % fetal bovine serum, 100 U/ml penicillin, and 100 μg/ml streptomycin at 37 °C in 5 % CO2 incubator. To synchronize the cells at prometaphase, they were treated with 50 ng/ml nocodazole for 16 h. |
Reaction Conditions | 50 ng/ml; 16h |
Applications | Approximately 50 % of the cells were synchronized in G2/M phases. |
| Animal experiment [2]: | |
Animal models | nude mouse |
Preparation Method | COLO 205 cells were injected subcutaneously between the scapulae of each nude mouse. Once tumors reached a mean size of 200mm3 , animals received intraperitoneal injections of DMSO (25µL), ketoconazole(50 mg/kg), nocodazole(5 mg/kg), or ketoconazole+nocodazole three times per week for 6 week. |
Dosage form | 5mg/kg; i.p. |
Applications | Nocodazole has antitumor effects in athymic mice bearing COLO 205 tumor xenografts. |
References: [1]Makiyama T, Obama T, Watanabe Y, et al. Behavior of intracellular lipid droplets during cell division in HuH7 hepatoma cells[J]. Experimental Cell Research, 2023, 433(2): 113855. [2]Wang Y J, Jeng J H, Chen R J, et al. Ketoconazole potentiates the antitumor effects of nocodazole: In vivo therapy for human tumor xenografts in nude mice[J]. Molecular Carcinogenesis: Published in cooperation with the University of Texas MD Anderson Cancer Center, 2002, 34(4): 199-210. | |
| Cas No. | 31430-18-9 | SDF | |
| Synonyms | NSC 238159, Oncodazole, R 17934 | ||
| Chemical Name | methyl N-[6-(thiophene-2-carbonyl)-1H-benzimidazol-2-yl]carbamate | ||
| Canonical SMILES | COC(=O)NC1=NC2=C(N1)C=C(C=C2)C(=O)C3=CC=CS3 | ||
| Formula | C14H11N3O3S | M.Wt | 301.32 |
| Solubility | ≥ 15.1mg/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 | 3.3187 mL | 16.5937 mL | 33.1873 mL |
| 5 mM | 0.6637 mL | 3.3187 mL | 6.6375 mL |
| 10 mM | 0.3319 mL | 1.6594 mL | 3.3187 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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