| CAS |
31430-18-9 |
| Chinese Name |
诺考达唑 |
| English Name |
Nocodazole |
| Synonyms |
Oncodazole;R17934 |
| Molecular Formula |
C14H11N3O3S |
| Molecular Weight |
301.32 |
| Solubility |
Soluble in DMSO |
| Purity |
≥98% |
| Appearance |
Light yellow to yellow Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 250-626-5 |
| MDL |
MFCD00005588 |
| SMILES |
O=C(OC)NC1=NC2=CC=C(C(C3=CC=CS3)=O)C=C2N1 |
| InChIKey |
KYRVNWMVYQXFEU-UHFFFAOYSA-N |
| InChI |
InChI=1S/C14H11N3O3S/c1-20-14(19)17-13-15-9-5-4-8(7-10(9)16-13)12(18)11-3-2-6-21-11/h2-7H,1H3,(H2,15,16,17,19) |
| PubChem CID |
4122 |
| Target Point |
Microtubule/Tubulin |
| Passage |
Cytoskeleton |
| Background |
Nocodazole is a rapidly reversible microtubule inhibitor. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly kinetics, thereby preventing mitosis and inducing tumor cell apoptosis. |
| Biological Activity |
Nocodazole是快速可逆的 microtubule 抑制剂。 Nocodazole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[1-6]。 |
| In Vitro |
Nocodazole(1 nM)诱导COLO 205癌细胞凋亡[4]。 Nocodazole(≥30μg/ mL)显著增加膜联蛋白-V结合细胞的百分比，而不显著改变人红细胞的平均前向散射[5]。Nocodazole对c-KIT表现出良好的亲和力，在高度恶性的人癌细胞中Kd值为1.6μM。诺考达唑对促分裂原活化蛋白激酶(MAPK)途径的组分显示出良好的结合亲和力，例如BRAF(Kd =1.8μM)，BRAF(V600E)(Kd =1.1μM)，MEK1(Kd =1.7μM)，和MEK2(Kd =1.6μM)[1]。 Nocodazole对αβIV的亲和力最高，对αβIII的亲和力最低[2]。从Nocodazole阻滞释放后，有丝分裂同步的细胞对非常低浓度的紫杉醇敏感，持续 90分钟[3]。 |
| In Vivo |
Nocodazole(5mg/kg /每周三次，ip)在携带COLO205肿瘤异种移植物的无胸腺小鼠中具有抗肿瘤作用。 Nocodazole(1 nM)+酮康唑可显著增加肿瘤组织中p21/CIP1和p27/KIP1蛋白的水平[4]。 |
| Cell Experiment |
蛋白质以50μg/泳道加载，并用12％(w：v)十二烷基硫酸钠 - 聚丙烯酰胺凝胶电泳分离，印迹，并用抗体对细胞周期蛋白E，p53，p21/CIP1，p27/KIP1，甘油醛-3-磷酸进行探测。脱氢酶(GAPDH)，细胞周期蛋白A，细胞周期蛋白D1，细胞周期蛋白D3，细胞周期蛋白B，CDK2，CDK4和细胞色素C.免疫反应条带通过与发色底物氮蓝四唑和5-溴-4-氯-3-吲哚 - 一起孵育而可视化。磷酸盐。 GAPDH的表达用作相等蛋白质加载的对照。 |
| Animal Experiment |
COLO 205细胞在补充有10％FCS的RPMI 1640中生长。通过连续两次胰蛋白酶消化收获细胞，以300×g离心;保持5分钟，洗涤两次，并重悬于无菌磷酸盐缓冲盐水(PBS)中。将0.1mL的细胞(5×105)皮下注射到每只裸鼠的肩胛骨之间。移植后，用卡尺测量肿瘤大小，估计肿瘤体积。一旦肿瘤达到平均大小200 mm3，动物每周三次腹膜内注射DMSO(25μL)，酮康唑(50 mg/kg)，诺考达唑(5 mg/kg)或酮康唑+诺考达唑，持续6周。 |
| Data Literature Source |
[1]. Park H，et al. Nocodazole is a high-affinity ligand for the cancer-related kinases ABL，c-KIT，BRAF，and MEK. ChemMedChem. 2012 Jan 2;7(1):53-6.
[2]. Keliang Xu，et al. Interaction of nocodazole with tubulin isotypes. Drug Development Research 2002
[3]. Long BH，et al. Paclitaxel inhibits progression of mitotic cells to G1 phase by interference with spindle formation without affecting other microtubule functions during anaphase and telephase. Cancer Res. 1994 Aug 15;54(16):4355-61.
[4]. Wang YJ，et al. Ketoconazole potentiates the antitumor effects of nocodazole: In vivo therapy for human tumor xenografts in nude mice. Mol Carcinog. 2002 Aug;34(4):199-210.
[5]. Signoretto E，et al. Nocodazole Induced Suicidal Death of Human Erythrocytes. Cell Physiol Biochem. 2016;38(1):379-92.
[6]. 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. |
| Unit |
Piece |
| Specification |
10mg 50mg |
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