Nocodazole
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Nocodazole是一种抗有丝分裂药物,是一种快速可逆的微管聚合抑制剂,在无细胞实验中抑制Abl、Abl(E255K)和Ab1(T315I)的IC50值分别为0.21 μM、0.53μM和0.64μM[ 1]。
体外实验:Nocodazole是癌症相关激酶的高亲和力配体,包括Abl磷酸化、c-Kit、BRAF和MEK,Kd值分别为0.091 μM、1.6 μM、1.8 μM和1.6 μM。此外,对Abl(E255K)磷酸化、Abl(T315I)磷酸化、BRAF(V600E)和PI3Kγ的Kd分别为0.12 μM、0.17 μM、1.1 μM和1.5 μM。在慢性淋巴细胞白血病细胞中,Nocodazole诱导细胞凋亡。在一些人类结肠癌细胞中,Nocodazole减少细胞凋亡。此外,Nocodazole抑制胰岛素刺激的葡萄糖转运。Nocodazole损害迁移的内侧胶质隆起细胞的形态和方向性[1]。高浓度Nocodazole快速解聚细胞中的微管,低浓度Nocodazole抑制微管动态不稳定性[2]。在SH-SY5Y细胞中,Nocodazole通过与β-微管蛋白结合而破坏微管,阻止两个链间二硫键中其中一个的形成,并损害囊泡的转运。Nocodazole显著减弱METH诱导的细胞死亡和溶酶体功能障碍[3]。Nocodazole(≥ 50 nM)导致成纤维细胞运动快速降低至新速率,维持大于2小时。Nocodazole(100 nM)使运动速率降低超过60%,300 nM的Nocodazole完全阻止细胞运动[4]。
在体实验:在携带COLO205肿瘤异种移植物的无胸腺小鼠中,Ketoconazole(50 mg/kg,每周三次)和Nocodazole(5 mg/kg,每周三次)治疗6周后,KT显著增强ND的抗肿瘤作用。与单独用Ketoconazole或Nocodazole治疗相比,小鼠的肿瘤体积和肿瘤重量显著降低。Nocodazole与Ketoconazole联合治疗显著增强用Ketoconazole或单独Nocodazole治疗的COLO 205肿瘤异种移植物的凋亡[5]。
参考文献:
[1]. Park H, Hong S, Hong S. Nocodazole is a High‐Affinity Ligand for the Cancer‐Related Kinases ABL, c‐KIT, BRAF, and MEK[J]. ChemMedChem, 2012, 7(1): 53-56.
[2]. Xu K, Schwarz P M, Luduea R F. Interaction of nocodazole with tubulin isotypes[J]. Drug development research, 2002, 55(2): 91-96.
[3]. Nara A, Aki T, Funakoshi T, et al. Hyperstimulation of macropinocytosis leads to lysosomal dysfunction during exposure to methamphetamine in SH-SY5Y cells[J]. Brain research, 2012, 1466: 1-14.
[4]. Liao G, Nagasaki T, Gundersen G G. Low concentrations of nocodazole interfere with fibroblast locomotion without significantly affecting microtubule level: implications for the role of dynamic microtubules in cell locomotion[J]. Journal of Cell Science, 1995, 108(11): 3473-3483.
[5]. Wang Y J, Jeng J H, Chen R J, et al. Ketoconazole potentiates the antitumor effects of nocodazole: In vivo therapy for human tumor xenografts in nude mice[J]. Molecular carcinogenesis, 2002, 34(4): 199-210.
- 1. Yongman Liu, Jianye Wang, et al. "Quantifying 3D cell–matrix interactions during mitosis and the effect of anticancer drugs on the interactions." Nano Research. ISSN 1998-0124 CN 11-5974/O4.
- 2. Wei P, Ning M, et al. "Spiroplasma eriocheiris entered Drosophila Schneider 2 cells and relied on clathrin-mediated endocytosis and macropinocytosis." Infect Immun. 2019 Aug 26. pii: IAI.00233-19. PMID:31451616
- 3. Wang H, Liu W, et al. "Inhibitor analysis revealed that clathrin-mediated endocytosis is involed in cellular entry of type III grass carp reovirus." Virol J. 2018 May 24;15(1):92. PMID:29793525
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 301.32 |
Cas No. | 31430-18-9 |
Formula | C14H11N3O3S |
Solubility | insoluble in H2O; insoluble in EtOH; ≥15.066 mg/mL in DMSO |
Chemical Name | methyl N-[6-(thiophene-2-carbonyl)-1H-benzimidazol-2-yl]carbamate |
SDF | Download SDF |
Canonical SMILES | COC(=O)NC1=NC2=C(N1)C=C(C=C2)C(=O)C3=CC=CS3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
SH-SY5Y细胞,NRK成纤维细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于15.1 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
25-400 nM,1 μM,30 min |
应用 |
在SH-SY5Y细胞中,Nocodazole(1 μM)通过结合β微管蛋白破坏微管,阻止两个链间二硫键中其中一个的形成,并阻碍囊泡的转运。Nocodazole显著减弱METH诱导的细胞死亡和溶酶体功能障碍。在大于2小时的Nocodazole治疗过程中,Nocodazole(400 nM)完全抑制细胞运动。Nocodazole以剂量依赖性方式降低运动速率。Nocodazole(25 nM、100 nM)显著抑制细胞运动。 |
动物实验 [2]: | |
动物模型 |
携带COLO 205肿瘤异种移植物的不孕小鼠 |
给药剂量 |
5 mg/kg,每周三次 |
应用 |
治疗6周后,nocodazole的抗肿瘤作用在小鼠中被ketoconazole显著增强。在接受这些治疗的小鼠中没有观察到毒性症状。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Liao G, Nagasaki T, Gundersen G G. Low concentrations of nocodazole interfere with fibroblast locomotion without significantly affecting microtubule level: implications for the role of dynamic microtubules in cell locomotion[J]. Journal of Cell Science, 1995, 108(11): 3473-3483. [2]. Liao G, Nagasaki T, Gundersen G G. Low concentrations of nocodazole interfere with fibroblast locomotion without significantly affecting microtubule level: implications for the role of dynamic microtubules in cell locomotion[J]. Journal of Cell Science, 1995, 108(11): 3473-3483. |
Description | Nocodazole is a potent and reversible inhibitor of tubulin production. | |||||
Targets | tubulin | |||||
IC50 |
质量控制和MSDS
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