诺考达唑, Nocodazole,31430-18-9

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抑制剂描述：

产品名称：Nocodazole

产品别名：见爱必信官网

英文别名：Nocodazole

靶点：Microtubule/Tubulin

CAS：31430-18-9

纯度：＞98%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

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。

溶解性：DMSO ：15.1 mg/mL (50 mM)

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.

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.

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