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Synonyms | R17934, Oncodazole, NSC238159 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C14H11N3O3S |
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分子量 | 301.32 | CAS No. | 31430-18-9 | |
Solubility (25°C)* | 体外 | DMSO | 7 mg/mL (23.23 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Nocodazole is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis. |
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in vitro | 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. [1] At high concentrations, Nocodazole rapidly depolymerizes microtubules in cells, while low concentrations of Nocodazole inhibit microtubule dynamic instability. [2] 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. [3] 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. [4] 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[6]. |
in vivo | 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. [5] |
細胞アッセイ | 細胞株 | H1975 cells |
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濃度 | 50 ng/ml | |
反応時間 | 24 h | |
実験の流れ | Cells were treated with indicated concentration of the drug for 24 hour. |
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動物実験 | 動物モデル | Nude mice with COLO-205 tumor xenografts |
投薬量 | 5 mg/kg | |
投与方法 | Administered via i.p. |
, , J Biol Chem, 2016, 291:14761-14772.
Data from [Data independently produced by , , Cancer Res, 2018, doi:10.1158/0008-5472.CAN-18-0520]
Data from [Data independently produced by , , Cell Signal, 2016, 28(12):1826-1832]
Nucleolar protein TAAP1/C22orf46 confers pro-survival signaling in non-small cell lung cancer [ Life Sci Alliance, 2024, 7(4)e202302257] | PubMed: 38228372 |
Allosteric regulation of CAD modulates de novo pyrimidine synthesis during the cell cycle [ Nat Metab, 2023, 5(2):277-293] | PubMed: 36747088 |
Real-Time Dissection of the Transportation and miRNA-Release Dynamics of Small Extracellular Vesicles [ Adv Sci (Weinh), 2023, 10(7):e2205566] | PubMed: 36599707 |
Harnessing transcriptionally driven chromosomal instability adaptation to target therapy-refractory lethal prostate cancer [ Cell Rep Med, 2023, 4(2):100937] | PubMed: 36787737 |
Loss of RanGAP1 drives chromosome instability and rapid tumorigenesis of osteosarcoma [ Dev Cell, 2023, 58(3):192-210.e11] | PubMed: 36696903 |
Fatty acid oxidation facilitates DNA double-strand break repair by promoting PARP1 acetylation [ Cell Death Dis, 2023, 14(7):435] | PubMed: 37454129 |
Targeting MCL-1 triggers DNA damage and an anti-proliferative response independent from apoptosis induction [ Cell Rep, 2023, 42(10):113176] | PubMed: 37773750 |
Ferroptosis signaling promotes the release of misfolded proteins via exosomes to rescue ER stress in hepatocellular carcinoma [ Free Radic Biol Med, 2023, 202:110-120] | PubMed: 36997100 |
PLK1 maintains DNA methylation and cell viability by regulating phosphorylation-dependent UHRF1 protein stability [ Cell Death Discov, 2023, 9(1):367] | PubMed: 37788997 |
PLK1 maintains DNA methylation and cell viability by regulating phosphorylation-dependent UHRF1 protein stability [ Cell Death Discov, 2023, 9(1):367] | PubMed: 37788997 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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