Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XMU-MP-1 是一种促凋亡、无菌的 20 样激酶 MST1 和 2 的抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 589 | 现货 | ||
2 mg | ¥ 861 | 现货 | ||
5 mg | ¥ 1,670 | 现货 | ||
10 mg | ¥ 2,960 | 现货 | ||
25 mg | ¥ 4,880 | 现货 | ||
50 mg | ¥ 6,990 | 现货 | ||
100 mg | ¥ 9,430 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,580 | 现货 |
产品描述 | XMU-MP-1 is an inhibitor of the pro-apoptotic, sterile 20-like kinases MST1 and 2. |
靶点活性 | MST2:38.1 nM, MST1:71.1 nM |
体外活性 | XMU-MP-1 reduces the phosphorylation of endogenous MOB1, LATS1/2, and YAP in HepG2 cells in a dose-dependent manner at concentrations ranging from 0.1 to 10 μM. XMU-MP-1 treatment inhibits hydrogen peroxide-stimulated MOB1 phosphorylation and MST1/2 autophosphorylation in a variety of cell lines, including mouse macrophage-like cells, human osteosarcoma, human colorectal adenocarcinoma cells. XMU-MP-1 blocks MST1/2 kinase activities, thereby activating the downstream effector Yes-associated protein and promoting cell growth. XMU-MP-1 can potently and reversibly suppress the activities of kinases MST1/2 and enhance their downstream YAP activation in cells. |
体内活性 | XMU-MP-1 displays excellent in in vivo pharmacokinetics and is able to augment mouse intestinal repair, as well as liver repair and regeneration, in both acute and chronic liver injury mouse models at a dose of 1 to 3 mg/kg via intraperitoneal injection. XMU-MP-1 treatment exhibited substantially greater repopulation rate of human hepatocytes in the Fah-deficient mouse model than in the vehicle-treated control, indicating that XMU-MP-1 treatment might facilitate human liver regeneration. Thus, the pharmacological modulation of MST1/2 kinase activities provides a novel approach to potentiate tissue repair and regeneration, with XMU-MP-1 as the first lead for the development of targeted regenerative therapeutics. |
激酶实验 | XMU-MP-1 is dissolved in DMSO (stock concentration, 10 mM). For the in vitro kinase inhibition assays, recombinant GST-tagged MOB1a and various forms of recombinant His-tagged full-length MST1 or MST2 kinase are expressed and purified from Escherichia coli. The assays are performed with the various doses of XMU-MP-1 in the kinase assay buffer for 30 min at 30°C[1]. |
分子量 | 416.48 |
分子式 | C17H16N6O3S2 |
CAS No. | 2061980-01-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12.5 mg/mL (30.01 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4011 mL | 12.0054 mL | 24.0108 mL | 60.0269 mL |
5 mM | 0.4802 mL | 2.4011 mL | 4.8022 mL | 12.0054 mL | |
10 mM | 0.2401 mL | 1.2005 mL | 2.4011 mL | 6.0027 mL | |
20 mM | 0.1201 mL | 0.6003 mL | 1.2005 mL | 3.0013 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。
XMU-MP-1 2061980-01-4 Stem Cells Hippo pathway XMU MP 1 Inhibitor Hippo (MST) inhibit XMUMP1 inhibitor