Nocodazole (CAS 31430-18-9) is an anti-mitotic small molecule commonly utilized in biomedical research as a potent and reversible inhibitor of microtubule polymerization. Its mechanism involves direct binding to β-tubulin, disrupting microtubule assembly and stability. It exhibits inhibitory effects on various kinases associated with oncogenesis, including Abl, c-Kit, BRAF, and MEK, and induces apoptosis in cancer cells. In vitro exposure at high concentrations rapidly depolymerizes microtubules, while lower concentrations primarily affect their dynamic instability. Nocodazole serves as a valuable tool in studies probing microtubule dynamics, intracellular trafficking, cell cycle regulation, and antitumor therapeutic evaluations.
References: [1]. Park H, Hong S, Hong S. Nocodazole is a High‐Affinity Ligand for the Cancer‐Related Kinases ABL, c‐KIT, BRAF, and MEK[J]. ChemMedChem, 2012, 7(1): 53-56. [2]. Xu K, Schwarz P M, Ludue a R F. Interaction of nocodazole with tubulin isotypes[J]. Drug development research, 2002, 55(2): 91-96. [3]. Nara A, Aki T, Funakoshi T, et al. Hyperstimulation of macropinocytosis leads to lysosomal dysfunction during exposure to methamphetamine in SH-SY5Y cells[J]. Brain research, 2012, 1466: 1-14. [4]. Liao G, Nagasaki T, Gundersen G G. Low concentrations of nocodazole interfere with fibroblast locomotion without significantly affecting microtubule level: implications for the role of dynamic microtubules in cell locomotion[J]. Journal of Cell Science, 1995, 108(11): 3473-3483. [5]. 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, 2002, 34(4): 199-210.
Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips
We do not recommend long-term storage for the solution, please use it up soon.
Protocol
Cell experiment [1]:
Cell lines
SH-SY5Y cells, NRK fibroblasts
Preparation method
The solubility of this compound in DMSO is >15.1 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition
25 nM to 400 nM, 1 μM; 30 min
Applications
In SH-SY5Y cells, Nocodazole (1 μM) disrupted microtubules by binding to β-tubulin, prevented the formation of one of the two interchain disulfide linkages and impaired the transport of vesicles. Nocodazole significantly attenuated METH-induced cell death and lysosomal dysfunction. Nocodazole (400 nM) completely inhibited cell locomotion that was maintained throughout the nocodazole treatment (>2 hours). Nocodazole treatment resulted in a dose-dependent decrease in the rate of locomotion. Nocodazole (25 nM, 100 nM) significantly inhibited cell locomotion.
Animal experiment [2]:
Animal models
Athymic mice bearing COLO 205 tumor xenografts
Dosage form
5 mg/kg/three times per week
Application
The antitumor effects of nocodazole were significantly potentiated by ketoconazole in mice after 6 wk of treatment. No gross signs of toxicity were observed in mice receiving these treatments.
Other notes
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References:
[1]. Liao G, Nagasaki T, Gundersen G G. Low concentrations of nocodazole interfere with fibroblast locomotion without significantly affecting microtubule level: implications for the role of dynamic microtubules in cell locomotion[J]. Journal of Cell Science, 1995, 108(11): 3473-3483.
[2]. Liao G, Nagasaki T, Gundersen G G. Low concentrations of nocodazole interfere with fibroblast locomotion without significantly affecting microtubule level: implications for the role of dynamic microtubules in cell locomotion[J]. Journal of Cell Science, 1995, 108(11): 3473-3483.
Biological Activity
Description
Nocodazole is a potent and reversible inhibitor of tubulin production.
Targets
tubulin
IC50
Quality Control
You might also be interested by the following products: