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Nocodazole

Nocodazole (Oncodazole) 是一种合成的微管聚合抑制剂。它抑制 Bcr-Abl，增强 CRISPR/Cas9的活性。它与β-微管蛋白结合并破坏微管组装/拆卸动力学，从而防止有丝分裂并诱导肿瘤细胞凋亡。

CAS号

31430-18-9

分子式

C14H11N3O3S

主要靶点

Autophagy|Apoptosis|CRISPR/Cas9|Bcr-Abl|Microtubule Associated

仅限科研使用

Cat No : CM05137

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Synonyms

Oncodazole|R17934|诺考达唑

验证数据展示

  • CAS No.: 31430-18-9

    Nocodazole
    CAS#: 31430-18-9

产品信息

Nocodazole is a synthetic inhibitor of microtubule polymerization, also inhibits Abl (IC50: 0.21 μM), Abl(E255K, IC50: 0.53 μM) and Abl(T315I, IC50: 0.64 μM) in cell-free assays. Nocodazole binds to beta-tubulin and disrupts microtubule assembly/disassembly dynamics.

CAS号 31430-18-9
分子式 C14H11N3O3S
主要靶点 Autophagy|Apoptosis|CRISPR/Cas9|Bcr-Abl|Microtubule Associated
主要通路 血管生成|蛋白酪氨酸激酶|细胞骨架|凋亡|自噬|DNA损伤和修复
分子量 301.32
纯度 99.34%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 Oncodazole|R17934|诺考达唑

靶点活性

Abl (E255K):0.53 μM|Abl:0.21 μM|Abl (T315I):0.64 μM

体内活性

Nocodazole与癌症相关激酶具有较高亲和力,如磷酸化ABL（Kd：0.091 μM）,c-KIT（Kd：1.6 μM）,BRAF（Kd：1.8 μM）和MEK（Kd：1.6 μM）。Nocodazole对ABL(E255K)磷酸化（Kd：0.12 μM）, ABL(T315I) 磷酸化（Kd：0.17 μM）,BRAF(V600E)（Kd：1.1 μM）和PI3Kγ（Kd：1.5 μM）的亲和性也很高。高浓度Nocodazole可使细胞中微管迅速解聚,而低浓度可抑制微管的动态不稳定。经Nocodazole同步化处理6 h的分裂期细胞,加入不同浓度的紫杉醇后,可使G1期阻滞（IC50：4 nM）。

体外活性

在COLO205肿瘤移植模型中,Nocodazole与酮康唑联用对凋亡的诱导效果有加强作用,对小鼠的肿瘤体积和重量也有更强地抑制效果.

溶解度

DMSO:15.1 mg/mL (50 mM)

细胞实验

Nocodazole is dissolved in a final concentration of 0.05% DMSO. 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.

参考文献

1.Park H, et al. ChemMedChem. 2012, 7(1), 53-56.
2.Bai Y, Wang W, Li S, et al. C1QBP Promotes Homologous Recombination by Stabilizing MRE11 and Controlling the Assembly and Activation of MRE11/RAD50/NBS1 Complex[J]. Molecular Cell. 2019.
3.Xu KL, et al. Drug Dev Res. 2002, 55(2), 91-96.
4.Long BH, et al. Cancer Res. 1994, 54(16), 4355-4361.
5.Nara A, et al. Brain Res. 2012.
6.Wang YJ, et al. Mol Carcinog. 2002, 34(4), 199-210.
7.Signoretto E, et al. Nocodazole Induced Suicidal Death of Human Erythrocytes. Cell Physiol Biochem. 2016;38(1):379-92.
8.Zhang JP, et al. 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.
9.Li X, Tang H, Huang X, et al. Rigidity‐Dependent Placental Cells Uptake of Silk‐Based Microcapsules[J]. Macromolecular bioscience. 2019: 1900105.
10.Reyes G X, Kolodziejczak A, Devakumar L J P S, et al. Ligation of newly replicated DNA controls the timing of DNA mismatch repair[J]. Current Biology.

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