Nocodazole

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Chemical Structure| 31430-18-9 同义名 : Oncodazole;R17934;NSC238159
CAS号 : 31430-18-9
货号 : A260772
分子式 : C14H11N3O3S
纯度 : 99%+
分子量 : 301.32
MDL号 : MFCD00005588
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(59.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 0.4 mg/mL clear

PO 0.5% CMC-Na 65 mg/mL suspension

生物活性
描述 Microtubules, part of the cytoskeleton that provides structure and shape to the cytoplasm of cells, are tubular polymers of tubulin formed by polymerization. Nocodazole is a standard anti-microtubule agent that interferes with the polymerization and now be mostly used as depolymerizing drug in basic cell biology research[8]. Nocodazole can be used as a high-affinity ligand for the cancer-related kinases including Abl phosphorylated, c-Kit, BRAF, and MEK. Furthermore, Nocodazole induces apoptosis in chronic lymphocytic leukemia cells, inhibits insulin-stimulated glucose transport and decreases apoptosis in some human colon carcinoma cells[9]. In vitro Tubulin Polymerization Assays, Nocodazole inhibited tumor cell lines including NCIH460, SKOV3, BT549,451LU, COLO-205 at 48h with IC50 values 68nM, 80nM, 69nM, 72nM, 88nM respectively, which was reflected by a decreased level of steady state turbidity in a dose-dependent manner[5]. To learn how the spindle assembly checkpoint (SAC) inhibitory is extinguished, 9A-Hec1-expressing cells exhibited a robust mitotic arrest after incubation in 5 mM nocodazole for 5 h. As comparison, WT-Hec1 was treated with a moderately low dose (300 nM) of nocodazole, which resulted in the loss of all non-kinetochore spindle microtubules but retention of kinetochore–microtubule[6]. In addition, nocodazole can also improve the CRISPR-mediated HDR efficiency, a 600-bp homology in both arms leads to high-level genome knock in, with 97–100% of the donor insertion events being mediated by HDR. The combined use of CCND1, a cyclin that functions in G1/S transition, and nocodazole, a G2/M phase synchronizer, doubles HDR efficiency to up to 30% in iPSCs, the results showed an additive effect on enhancing precise genome editing[7].
作用机制 Nocodazole will bind to β-Tb and block polymerization, arrest mammalian cells in mitosis and release them into cytokinesis and G1 as well as mis-regulate mitotic kinases[8].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human 451LU cells Proliferation assay 48 h Antiproliferative activity against human 451LU cells after 48 hrs by alamar blue assay, IC50=72 nM 21563750
human A549 cells Proliferation assay 48 h Antiproliferative activity against human A549 cells after 48 hrs by SRB assay, GI50=20 nM 25827522
human A549 cells Cytotoxic assay 24 h Cytotoxicity against human A549 cells after 24 hrs by MTT assay, IC50=36.6 nM 20110137
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.32mL

0.66mL

0.33mL

16.59mL

3.32mL

1.66mL

33.19mL

6.64mL

3.32mL
参考文献

[1]7(1):53-6. doi: 10.1002/cmdc.201100410. Epub 2011 Oct 14.

[2]7(1):53-6. doi: 10.1002/cmdc.201100410. Epub 2011 Oct 14.

[3]54(12):4247-63. doi: 10.1021/jm200436t. Epub 2011 May 26.

[4]6:10036. doi: 10.1038/ncomms10036

[5]Prinz H. N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. J Med Chem. 2011 Jun 23;54(12):4247-63. doi: 10.1021/jm200436t. Epub 2011 May 26.

[6]Tauchman EC. Stable kinetochore-microtubule attachment is sufficient to silence the spindle assembly checkpoint in human cells. Nat Commun. 2015 Dec 1;6:10036. doi: 10.1038/ncomms10036

[7]Zhang JP. Efficient precise knockin with a double cut HDR donor after CRISPR/Cas9-mediated double-stranded DNA cleavage. Genome Biol. 2017 Feb 20;18(1):35. doi: 10.1186/s13059-017-1164-8.