1. Cell Cycle/DNA Damage
    Cytoskeleton
    Protein Tyrosine Kinase/RTK
    Autophagy
    Apoptosis
  2. Microtubule/Tubulin
    Bcr-Abl
    CRISPR/Cas9
    Autophagy
    Apoptosis
  3. Nocodazole

Nocodazole (Synonyms: Oncodazole; R17934)

Cat. No.: HY-13520 Purity: 98.68%
Handling Instructions

Nocodazole is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, activates CRISPR/Cas9.

For research use only. We do not sell to patients.

Nocodazole Chemical Structure

Nocodazole Chemical Structure

CAS No. : 31430-18-9

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Based on 9 publication(s) in Google Scholar

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Description

Nocodazole is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, activates CRISPR/Cas9.

IC50 & Target[1]

Abl

91 nM (Kd)

ABL(E255K)

120 nM (Kd)

ABL(T315I)

170 nM (Kd)

BRAF

1.8 μM (Kd)

BRAF(V600E)

1.1 μM (Kd)

c-KIT

1.6 μM (Kd)

MEK1

1.7 μM (Kd)

MEK2

1.6 μM (Kd)

MET

1.7 μM (Kd)

PI3Kγ

1.5 μM (Kd)

Microtubule/Tubulin

 

CRISPR/Cas9

 

In Vitro

Nocodazole exhibits good affinity toward c-KIT, with a Kd value of 1.6 μM in highly malignant human cancer cells. Nocodazole displays good binding affinity toward the components of the mitogen-activated protein kinase (MAPK) pathway, such as BRAF (Kd=1.8 μM), BRAF(V600E) (Kd=1.1 μM), MEK1 (Kd=1.7 μM), and MEK2 (Kd=1.6 μM)[1]. Nocodazole has the highest affinity for αβIV and the lowest affinity for αβIII[2]. After release from the nocodazole block, cells synchronized in mitosis remaine sensitive to very low concentrations of paclitaxel for < 30 min, the time required for spindle formation, yet remains sensitive to vinblastine for > 90 min[3]. Nocodazole (1 nM) induces apoptosis of COLO 205 cancer cells[4]. Nocodazole (≥ 30 µg/mL) significantly increases the percentage of annexin-V-binding cells without significantly modifying average forward scatter of human erythrocytes[5].

In Vivo

Nocodazole (5 mg/kg/three times per week, i.p.) has antitumor effects in athymic mice bearing COLO 205 tumor xenografts. Nocodazole (1 nM) + ketoconazole dramatically increase the levels of p21/CIP1 and p27/KIP1 protein in the tumor tissues[4].

Molecular Weight

301.32

Formula

C₁₄H₁₁N₃O₃S

CAS No.

31430-18-9

SMILES

O=C(OC)NC1=NC2=CC=C(C(C3=CC=CS3)=O)C=C2N1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (66.37 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2 mg/mL (6.64 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[4]

Proteins are loaded at 50 μg/lane and separated by 12% (w:v) sodium dodecyl sulfate-polyacrylamide gel electrophoresis, blotted, and probed with antibodies for cyclin E, p53, p21/CIP1, p27/KIP1, glyceraldehyde 3-phosphate dehydrogenase (GAPDH), cyclin A, cyclin D1, cyclin D3, cyclin B, CDK2, CDK4, and cytochrome C. Immunoreactive bands are visualized by incubating with the colorigenic substrates nitroblue tetrazolium and 5-bromo-4-chloro-3-indolyl-phosphate. The expression of GAPDH is used as the control for equal protein loading.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

COLO 205 cells are grown in RPMI 1640 supplemented with 10% FCS. Cells are harvested through two consecutive trypsinizations, centrifuged at 300×g; for 5 min, washed twice, and resuspended in sterile phosphate-buffered saline (PBS). Cells (5×105) in 0.1 mL are injected subcutaneously between the scapulae of each nude mouse. After transplantation, tumor size is measured with calipers, and the tumor volume is estimated. Once tumors reach a mean size of 200 mm3, animals receive intraperitoneal injections of DMSO (25 μL), ketoconazole (50 mg/kg), nocodazole (5 mg/kg), or ketoconazole + nocodazole three times per week for 6 wk.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Nocodazole
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