1. Stem Cell/Wnt
  2. Hippo (MST)
  3. XMU-MP-1

XMU-MP-1 

目录号: HY-100526 纯度: 99.51%
产品使用指南

XMU-MP-1是可逆和选择性的 MST1/2 抑制剂,IC50 分别为71.1和38.1 nM。

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XMU-MP-1 Chemical Structure

XMU-MP-1 Chemical Structure

CAS No. : 2061980-01-4

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10 mM * 1 mL in DMSO ¥1924
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2 mg ¥1100
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5 mg ¥2100
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10 mg ¥3700
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25 mg ¥6900
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50 mg ¥12000
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100 mg ¥21000
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Top Publications Citing Use of Products

    XMU-MP-1 purchased from MCE. Usage Cited in: Cell Rep. 2017 Dec 19;21(12):3612-3623.

    Control and SLMAP mutant HAP1 cells are probed for phosphorylation of MST1/2 (T183/180), YAP (S127 and S397) and MOB1 (T35). Note increased phosphorylation of these proteins in the SLMAP mutant cells, which is completely suppressed by XMU-MP-1.

    XMU-MP-1 purchased from MCE. Usage Cited in: Nat Immunol. 2017 Sep;18(9):973-984.

    Spp1 expression in BMMs cultured (1×105 per well) in flat- or round-bottomed plates (horizontal axis) with (XMU-MP-1) or without (Vehicle) an inhibitor of Mst1 and Mst2 (5 μg/mL); results are presented relative to those of vehicle-treated cells cultured on flat-bottomed plates.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50s of 71.1 and 38.1 nM, respectively[1].

    IC50 & Target

    IC50: 71.1 (MST1), 38.1 nM (MST2)[1]

    体外研究
    (In Vitro)

    At concentrations ranging from 0.1 to 10 μM, XMU-MP-1 reduces the phosphorylation of endogenous MOB1, LATS1/2, and YAP in HepG2 cells in a dose-dependent manner. 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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    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. XMUMP-1 treatment exhibits 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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    416.48

    Formula

    C17H16N6O3S2

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 8 mg/mL (19.21 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4011 mL 12.0054 mL 24.0108 mL
    5 mM 0.4802 mL 2.4011 mL 4.8022 mL
    10 mM 0.2401 mL 1.2005 mL 2.4011 mL
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.83 mg/mL (1.99 mM); Clear solution

      此方案可获得 ≥ 0.83 mg/mL (1.99 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 0.83 mg/mL (1.99 mM); Clear solution

      此方案可获得 ≥ 0.83 mg/mL (1.99 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 0.83 mg/mL (1.99 mM); Clear solution

      此方案可获得 ≥ 0.83 mg/mL (1.99 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 4.

      请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 0.4 mg/mL (0.96 mM); Clear solution

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献
    Kinase Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    纯度: 99.51%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    XMU-MP-1
    目录号:
    HY-100526
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