1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Epigenetics Stem Cell/Wnt Apoptosis
  2. EGFR JAK STAT Apoptosis
  3. MRC-G-001

MRC-G-001 是一种 Genipin (HY-17389) 衍生物,其对于 A549 癌症细胞的 IC50 值为 117 μM。MRC-G-001 能抑制 EGFRJAK1STAT3 的磷酸化,并调节与上皮-间质转化 (EMT) 相关的蛋白质表达,从而抑制细胞迁移和侵袭。MRC-G-001 可诱导细胞周期停滞和细胞凋亡 (apoptosis)。MRC-G-001 可用于非小细胞肺癌等癌症的研究。

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MRC-G-001

MRC-G-001 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MRC-G-001 is a Genipin (HY-17389) derivative with an IC50 of 117 μM against A549 cancer cells. MRC-G-001 inhibits the phosphorylation of EGFR, JAK1, and STAT3, and modulates epithelial-mesenchymal transition (EMT)-related protein expression, thereby attenuating cell migration and invasion. MRC-G-001 induces cell cycle arrest and cell apoptosis. MRC-G-001 can be used for the study of cancers such as non-small-cell lung cancer[1].

IC50 & Target[1]

JAK1

 

STAT3

 

体外研究
(In Vitro)

MRC-G-001 (Compound 2b) (0-500 μM,24-72 h) 可使 A549 的细胞活力呈剂量和时间依赖性降低,与 Genipin 相比具有更强的细胞毒性[1]
MRC-G-001 (0-100 μM, 7 days) 能有效抑制 A549 细胞的长期增殖能力[1]
MRC-G-001 (0-250 μM) 可强效将 A549 细胞周期阻滞在 G1/S 期[1]
MRC-G-001 (0-250 μM, 24 h) 比 Genipin 更大程度上诱导了 A549 细胞凋亡[1]
MRC-G-001 (0-250 μM, 24 h) 能在 A549 细胞中有效抑制 EGFR 和 JAK1/STAT3 信号通路[1]
MRC-G-001 (100 μM, 0-24 h) 可通过干扰 TGF-β 诱导的 EMT 信号通路抑制 A549 细胞的迁移和侵袭[1]
MRC-G-001 在 A549 细胞中不抑制 ATP 依赖的 EGFR 激酶活性,但会结合 EGFR 的胞外域 (III 结构域),提示其可能通过一种替代性的非 ATP 依赖机制发挥作用,该机制或许与干扰 EGF 结合有关[1]

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

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0, 62.5, 125 and 250 μM
Incubation Time: 24 h
Result: Decreased the phosphorylated p-Rb (Ser807/811) level.
Increased the level of cleaved caspase-3, cleaved caspase-8, and cleaved caspase-9.
Resulted in effective suppression of p-EGFR, p-JAK1, and p-STAT3 protein expression levels.
Did not alter UCP2 expression at lower concentrations, but slightly decreased its level at 250 μM.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 0, 62.5, 125 and 250 μM
Incubation Time: 24 h
Result: Led to a dose-dependent increase in both early apoptotic and late apoptotic populations.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 100 μM
Incubation Time: 24 h
Result: Led to an upregulation of E-cadherin and downregulation of N-cadherin, MMP9, Snail, and RhoA.
Inhibited the phosphorylation of SMAD2 and SMAD3, while SMAD4 protein levels remained largely unchanged.
分子量

357.44

Formula

C21H27NO4

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
  • 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 *
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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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产品名称:
MRC-G-001
目录号:
HY-175009
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