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Locostatin

Locostatin

产品编号 T8823   CAS 133812-16-5

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。

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Locostatin Chemical Structure
Locostatin, CAS 133812-16-5
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: Locostatin (T8823)
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生物活性
化学信息
存储 & 溶解度
参考文献
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].
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].
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMF: 5 mg/ml

DMSO: 5 mg/ml

ethanol: 10 mg/ml

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TargetMol Library Books参考文献

1. A M J , Stefania Greco A , B M S I A , et al. Locostatin, a disrupter of Raf kinase inhibitor protein, inhibits extracellular matrix production, proliferation, and migration in human uterine leiomyoma and myometrial cells[J]. Fertility and Sterility, 2016, 106( 6):1530-1538. 2. Junji, Yuzi, Qiu, et al. Locostatin Alleviates Liver Fibrosis Induced by Carbon Tetrachloride in Mice.[J]. Digestive diseases and sciences, 2019.

TargetMol Library Books文献引用

1. Ye J J, Wei S L, Wei Y Y, et al.RKIP suppresses the influenza A virus‑induced airway inflammatory response via the ERK/MAPK pathway.International Journal of Molecular Medicine.2023, 51(1): 1-14.
Kobe2602 Regorafenib B-Raf IN 13 SGX-523 BAY-293 AZ 628 NSC-70220 GNE-9815

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 经典已知活性库 抗卵巢癌化合物库 抗胰腺癌化合物库 抗前列腺癌化合物库 MAPK 抑制剂库 NO PAINS 化合物库 HIF-1化合物库 抗肥胖化合物库 激酶抑制剂库

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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。

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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。

Keywords

Locostatin 133812-16-5 MAPK Raf Inhibitor inhibitor inhibit

 

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