2. Stem Cell/Wnt Apoptosis
  3. Hippo (MST) Caspase Bcl-2 Family Apoptosis
  4. MST3-IN-1

MST3-IN-1 是一种选择性并且具有口服活性的 MST3 抑制剂，其 IC50 值为122.4 nM。MST3-IN-1 对HepG2 细胞表现出抗增殖活性，能有效诱导 HepG2 细胞凋亡 (apoptosis)，并将细胞周期阻滞在 G2/M 期。MST3-IN-1 在 HepG2 异种移植小鼠模型中显著抑制肿瘤生长。MST3-IN-1 可用于肝癌的相关研究。

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MST3-IN-1 Chemical Structure

MST3-IN-1 Chemical Structure

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MST3-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MST3-IN-1 is an selective and orally active MST3 inhibitor, with an IC50 of 122.4 nM. MST3-IN-1 shows antiproliferative activity against HepG2 cell. MST3-IN-1 effectively induces apoptosis in HepG2 cells, and halts the cell cycle at the G2/M transition. MST3-IN-1 significantly suppressed tumor growth in HepG2 xenograft mice. MST3-IN-1 can be used for the study of liver cancer[1].

体外研究
(In Vitro)

MST3-IN-1 (Compound LD-1) (72 h) 对多种癌细胞系表现出抗增殖活性，其 GI50 值分别为0.68 μM (HepG2 细胞)、0.77 μM (HCT116 细胞) 和0.83 μM (H226 细胞)，对 HK2 细胞的抑制作用均大于 30 μM，表现出良好的选择性[1]。
MST3-IN-1 (1 μM) 对 MST3 的抑制率高达 95.49%，而对AKT2 的抑制率仅为66.51%[1]。
MST3-IN-1 (0.25-2 μM, 24 h) 可诱导 HepG2 细胞凋亡，并可能通过阻滞G2/M期抑制细胞增殖[1]。
MST3-IN-1 (0.33-3 μM, 24 h) 能以浓度依赖性方式降低 p-MST3 的表达水平，但不影响 MST3 的总蛋白表达[1]。

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

MST3-IN-1 相关抗体:

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Induced apoptosis in HepG2 cells.

Immunofluorescence[1]

Cell Line: HepG2 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Revealed distinct morphological characteristics of apoptosis, including chromatin condensation and nuclear fragmentation.

Cell Cycle Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.25, 0.5, 1 μM
Incubation Time: 24 h
Result: Increased the proportion of cells at the G2/M phase.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.33, 1, 3 μM
Incubation Time: 24 h
Result: Reduced the expression level of p-MST3.
Increased the expression level of cleaved caspase-3.
Reduced the expression levels of caspase-3 and Bcl-2.
Did not affect the expression level of MST3.
体内研究
(In Vivo)

MST3-IN-1 (Compound LD-1) (40 mg/kg，每日灌胃给药，持续 15 天) 在 HepG2 异种移植小鼠模型中显示出良好的抑制肝细胞癌肿瘤生长的疗效[1]。

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

Animal Model: HepG2 cells (5 × 106) were injected subcutaneously into the right armpit of the mice[1]
Dosage: 40 mg/kg
Administration: i.g. daily for 15 days
Result: Exhibited a significant tumor growth inhibition (TGI) rate of 47.64 %, outperforming the current first-line treatment agent Sorafenib (HY-10201) (TGI = 32.52 %).
Showed no mouse mortality or significant body weight loss was observed across all dosage groups.
分子量

547.52

Formula

C25H21F4N5O3S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MST3-IN-1 相关分类

  • 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)

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

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MST3-IN-1Hippo (MST)CaspaseBcl-2 FamilyApoptosisMST3cancerHepG2 cellsInhibitorinhibitorinhibit

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