Nocodazole 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。

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.

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.

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）。

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.

31430-18-9

C14H11N3O3S

301.32

诺考达唑;R17934;Oncodazole

DMSO:15.1 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years