Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Locostatin 是一种有效的细胞渗透性 Raf 激酶抑制剂蛋白 (RKIP)/Raf1 激酶相互作用抑制剂和细胞迁移抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 287 | 现货 | ||
10 mg | ¥ 428 | 现货 | ||
25 mg | ¥ 735 | 现货 | ||
50 mg | ¥ 1,090 | 现货 | ||
100 mg | ¥ 1,650 | 现货 | ||
200 mg | ¥ 2,470 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 297 | 现货 |
产品描述 | Locostatin is a potent and cell permeable inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration. |
体外活性 |
Locostatin treatment resulted in the activation of the mitogen-activated protein kinase (MAPK) signal pathway (ERK phosphorylation), providing a powerful validation of our targeting protocol. Further, RKIP inhibition by locostatin reduces ECM components. Moreover, the inhibition of RKIP by locostatin impaired cell proliferation and migration in both leiomyoma and myometrial cells. Finally, locostatin treatment reduced GSK3β expression. Therefore, even if the activation of MAPK pathway should increase proliferation and migration, the destabilization of GSK3β leads to the reduction of proliferation and migration of myometrial and leiomyoma cells[1].
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体内活性 |
Compared to the CCl4 group, HYP (208.56 ± 6.12) μg/g, percentage of total collagen at overall region (1.91 ± 0.13), MMP-13/TIMP-1 (0.19 ± 0.01), MPO (1.45 ± 0.04) U/g, TGF-β (2652 ± 91.20), PDGF-AA (3897 ± 290.69), and E-selectin (1569 ± 66.48) in the liver tissues were decreased significantly in the locostatin-treated group[2].
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动物实验 | Carbon tetrachloride (CCl4) was used to induce liver fibrosis in mice, and locostatin was injected intraperitoneally. Liver fibrosis was assessed by Masson and Sirius red staining, hydroxyproline (HYP) assay, and collagen percentage area. Collagen I, collagen III, and α-SMA were detected by RT-PCR and western blot. The levels of MMP-13, MMP-2, TIMP-1, and TIMP-2 were estimated by ELISA. Liver inflammation was evaluated by HE staining and immunohistochemistry; liver myeloperoxidase (MPO), superoxide dismutase, and malondialdehyde were measured by ELISA; and cytokines were by Mouse Cytokine Array Q4000[2] |
分子量 | 245.27 |
分子式 | C14H15NO3 |
CAS No. | 133812-16-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMF: 5 mg/ml
DMSO: 5 mg/ml
ethanol: 10 mg/ml
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Locostatin 133812-16-5 MAPK Raf Inhibitor inhibitor inhibit