1. Apoptosis
  2. MDM-2/p53 Apoptosis
  3. MDMX/MDM2-IN-2

MDMX/MDM2-IN-2 是一种有效的 p53-MDM2/MDMX 双重抑制剂,对 MDM2 和 MDMX 的 Ki 分别为 0.23 μM 和 2.45 μM。MDMX/MDM2-IN-2 抑制 p53 和 MDM2 蛋白的结合。MDMX/MDM2-IN-2 恢复 p53 的功能并使细胞周期停滞和细胞凋亡。MDMX/MDM2-IN-2 抑制细胞迁移和侵袭,具有抗肿瘤活性。

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MDMX/MDM2-IN-2 Chemical Structure

MDMX/MDM2-IN-2 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MDMX/MDM2-IN-2 is a potent p53-MDM2/MDMX dual inhibitors with Kis of 0.23 μM and 2.45 μM for MDM2 and MDMX, respectively. MDMX/MDM2-IN-2 inhibits the binding of p53 and MDM2 proteins. MDMX/MDM2-IN-2 restores the function of p53 and enables cell cycle arrest and apoptosis. MDMX/MDM2-IN-2 inhibits cell migration and invasion. MDMX/MDM2-IN-2 has antitumor activity[1].

IC50 & Target

Ki: 0.23 μM (MDM2) and 2.45 μM (MDMX)[1]

体外研究
(In Vitro)

MDMX/MDM2-IN-2 对 HCT116 和 SH-SY5Y 细胞表现出适度的抗增殖活性 (IC50 分别为 0.68 μM 和 0.54 μM)。MDMX/MDM2-IN-2 对正常人肺上皮 BEAS-2B 细胞和 LO2 肝细胞具有低细胞毒性 (IC50 分别为 17.96 μM 和 15.93 μM)[1]
MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 小时) 诱导 HCT116 和 SH-SY5Y 细胞凋亡[1]
MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 小时) 使细胞周期停滞在 G1 期[1]
MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 小时) 增加 p53 及其下游靶标 MDM2、MDMX、p21 和 cleaved-caspase3 的水平[1]
MDMX/MDM2-IN-2 (0.4-0.8 μM) 显着抑制 HCT116 和 SH-SY5Y 细胞的集落形成、迁移和侵袭[1]

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

Apoptosis Analysis[1]

Cell Line: HCT116 and SH-SY5Y cells
Concentration: 0.6, 1.2, 2.4 μM
Incubation Time: 48 h
Result: The percentages of apoptotic HCT116 and SH-SY5Y cells were 13.63% and 15.69% with 0.6 μM.
The percentage of apoptotic cells correspondingly increased to 37.6% and 40.8% with 2.4 μM.

Cell Cycle Analysis[1]

Cell Line: HCT116 and SH-SY5Y cells
Concentration: 0.6, 1.2, 2.4 μM
Incubation Time: 48 h
Result: There was an increase in the percentage of cancer cells at the G1 phase. Meanwhile, the percentage of G2 phase cells was relatively decreased.

Western Blot Analysis[1]

Cell Line: HCT116 and SH-SY5Y cells
Concentration: 0.6, 1.2, 2.4 μM
Incubation Time: 48 h
Result: Increased the levels of p53 and its downstream targets, MDM2, MDMX, p21 and cleaved-caspase3.

Cell Migration Assay [1]

Cell Line: HCT116 and SH-SY5Y cells
Concentration: 0.4, 0.6, 0.8 μM
Incubation Time: 48 h
Result: Significantly inhibited the migration and invasion in a dose-dependent manner.
分子量

576.87

Formula

C28H25Cl3FN3O3

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

MDMX/MDM2-IN-2 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)

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
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.

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MDMX/MDM2-IN-2
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