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  • Nocodazole
  • 诺考达唑;Oncodazole;R17934
  • 货号: abs817886
    CAS号: 31430-18-9
    分子式: C14H11N3O3S
    分子量: 301.32
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    货号-规格 货期 价格 数量
    abs817886-10mg 现货 ¥559.00
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    abs817886-50mg 现货 ¥1986.00
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    abs817886-100mg 现货 ¥3383.00
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    ! 该货号为 abs47029856 的新货号。
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    产品描述
    描述

    Nocodazole是一种微管聚合的快速可逆抑制剂,也抑制Abl, Abl(E255K)和Abl(T315I),IC50分别为0.21 μM, 0.53 μM和0.64 μM。

    纯度
    >98%
    储存/保存方法
    Store at -20°C
    基本信息
    别名
    诺考达唑;Oncodazole;R17934
    外观
    white to beige powder
    可溶性/溶解性
    DMSO :15.1 mg/mL (50 mM)
    生物活性
    靶点
    Microtubules,Abl,Abl (E255K),Abl (T315I)
    In vitro(体外研究)
    Nocodazole is a high-affinity ligand for the cancer-related kinases including Abl phosphorylated, c-Kit, BRAF, and MEK with Kd of 0.091 μM, 1.6 μM, 1.8 μM and 1.6 μM, respectively. In addition, the Kd of Nocodazole for Abl(E255K) phosphorylated, Abl(T315I) phosphorylated, BRAF(V600E) and PI3Kγ is 0.12 μM, 0.17 μM, 1.1 μM and 1.5 μM, respectively. Nocodazole induces apoptosis in chronic lymphocytic leukemia cells. Nocodazole inhibits insulin-stimulated glucose transport. Nocodazole decreases apoptosis in some human colon carcinoma cells. Nocodazole impairs the morphology and directionality of migrating medial gan-glionic eminence cells. At high concentrations, Nocodazole rapidly depolymerizes microtubules in cells, while low concentrations of Nocodazole inhibit microtubule dynamic instability. Mitotic cells incubated with different concentrations of Paclitaxel are inhibited from progressing to G1 phase 6 hours after release from the Nocodazole block, with a median inhibitory concentration of 4 nM. Nocodazole-pretreated cells exposed to Paclitaxel in the absence of Nocodazole only form free-floating microtubules, whereas pretreated cells exposed to Paclitaxel in the presence of Nocodazole-assembled centrosome organize microtubules. Nocodazole disrupts microtubules by binding to β-tubulin. Nocodazole prevents the formation of one of the two interchain disulfide linkages. Nocodazole impairs the transport of vesicles. Nocodazole suppress METH-induced cell death and lysosomal dysfunction. METH-induced cell death is significantly decreased by Nocodazole pretreatment in comparison to METH alone. Nocodazole doubles HDR efficiency to up to 30% in iPSCs. It improves the CRISPR-mediated HDR efficiency and has an additive effect on enhancing precise genome editing.
    In vivo(体内研究)
    The tumor volume and tumor weight of the mice treated with Ketoconazole  plus  Nocodazole are significantly reduced as compared with those treated with Ketoconazole or Nocodazole alone. Combined treatment with Ketoconazole  plus  Nocodazole strongly enhances apoptosis of COLO 205 tumor xenografts treated with Ketoconazole  or  Nocodazole alone.
    参考文献
    参考文献
    [1] Park H, et al. ChemMedChem. 2012, 7(1), 53-56.
    [2] Hoebeke, J., et al. 1976. Biochem. Biophys. Res. Commun. 69: 319-324.
    [3] Lin et al (2014) Enhanced homology-directed human genome engineering by controlled timing of CRISPR/Cas9 delivery. Elife 3 e04766.
    [4] Mizushima et al (2010) Methods in mammalian autophagy research. Cell 140 313.
    [5] Webb et al (2004) Microtubule disruption inhibits autophagosome-lysosome fusion: implications for studying the roles of aggresomes in polyglutamine diseases. Int.J.Biochem.Cell Biol. 36 2541.
    [6] Vasquez et al (1997) Nanomolar concentrations of nocodazole alter microtubule dynamic instability in vivo and in vitro. Mol.Biol.Cell 8 973.
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