Nocodazole (Synonyms: 諾考達唑; Oncodazole; R17934)
Nocodazole (Oncodazole) 是快速可逆的 microtubule 抑制劑。 Nocodazole與β-微管蛋白結(jié)合并破壞微管組裝/拆卸動力學(xué)，從而防止有絲分裂并誘導(dǎo)腫瘤細胞凋亡。Nocodazole 抑制 Bcr-Abl，增強 CRISPR/Cas9 的活性。
生物活性
Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
體外研究(In Vitro)
Nocodazole exhibits good affinity toward c-KIT, with a Kd value of 1.6?μM in highly malignant human cancer cells. Nocodazole displays good binding affinity toward the components of the mitogen-activated protein kinase (MAPK) pathway, such as BRAF (Kd=1.8?μM), BRAF(V600E) (Kd=1.1?μM), MEK1 (Kd=1.7?μM), and MEK2 (Kd=1.6?μM)[1]. Nocodazole has the highest affinity for αβIV and the lowest affinity for αβIII[2].
Nocodazole (1 nM) induces apoptosis of COLO 205 cancer cells[3].
Nocodazole (≥ 30 µg/mL) significantly increases the percentage of annexin-V-binding cells without significantly modifying average forward scatter of human erythrocytes[4].
In CHO cells, the addition of 1 nM Nocodazole, a concentration that suppresses microtubule dynamics, slows migration and increases the frequency and duration of resting states, but the directionality of the cells is maintained. In contrast to the effects of the low drug concentration, the addition of 70 nM Nocodazole, a concentration that eliminates the microtubule network, causes cells to move much more randomly, i.e., the directionality of the cells toward the wound is lost[6].
體內(nèi)研究(In Vivo
Nocodazole (5 mg/kg/three times per week, i.p.) has antitumor effects in athymic mice bearing COLO 205 tumor xenografts. Nocodazole (1 nM) + R-41400 dramatically increase the levels of p21/CIP1 and p27/KIP1 protein in the tumor tissues[3].
分子量：301.32
性狀：
Solid |
Formula：C14H11N3O3S
CAS 號：31430-18-9
中文名稱：諾考達唑
運輸條件
Room temperature in continental US; may vary elsewhere.
儲存方式
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 20 mg/mL (66.37 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3187 mL | 16.5937 mL | 33.1873 mL |
| 5 mM | 0.6637 mL | 3.3187 mL | 6.6375 mL |
| 10 mM | 0.3319 mL | 1.6594 mL | 3.3187 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： 50% PEG300 50% saline
Solubility: 5 mg/mL (16.59 mM); Suspended solution; Need ultrasonic
- 2.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2 mg/mL (6.64 mM); Clear solution
參考文獻
[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. [Content Brief]
[2]. Keliang Xu, et al. Interaction of nocodazole with tubulin isotypes. Drug Development Research 2002
[3]. Wang YJ, et al. R-41400 potentiates the antitumor effects of nocodazole: In vivo therapy for human tumor xenografts in nude mice. Mol Carcinog. 2002 Aug;34(4):199-210. [Content Brief]
[4]. Signoretto E, et al. Nocodazole Induced Suicidal Death of Human Erythrocytes. Cell Physiol Biochem. 2016;38(1):379-92. [Content Brief]
[5]. 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. [Content Brief]
[6]. Anutosh Ganguly, et al. The role of microtubules and their dynamics in cell migration. J Biol Chem. 2012 Dec 21;287(52):43359-69. [Content Brief]
注：產(chǎn)品僅用于科研
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