2. Cell Cycle/DNA Damage Epigenetics
  3. Aurora Kinase
  4. AurkA allosteric-IN-1

AurkA allosteric-IN-1 (compound 6h) 是 Aurora A (AurkA) 抑制剂 (IC50: 6.50 μM)，可抑制 Aurora A 的催化活性和非催化功能。Aurora A 调节双极有丝分裂纺锤体的组装和有丝分裂过程中染色体分离的保真度，具有非催化功能。AurkA allosteric-IN-1 通过结合 AurkA 的 Y 口袋，阻碍 AurkA 与激活因子 TPX2 的相互作用。

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AurkA allosteric-IN-1 Chemical Structure

AurkA allosteric-IN-1 Chemical Structure

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AurkA allosteric-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC50: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA[1].

IC50 & Target

Aurora A

6.5 μM (IC50, [1])

体外研究
(In Vitro)

AurkA allosteric-IN-1 (100 μM; 48 h) 在不同细胞类型间 (包括肺癌细胞系和直肠癌细胞系) 差异诱导了对细胞周期的阻滞作用[1]。
AurkA allosteric-IN-1 (20 μM; 48 h) 可下调癌细胞中磷酸组蛋白 H3 的水平[1]。
AurkA allosteric-IN-1 (25-400 μM; 48 h) 对 HeLa 细胞表现出显著抗细胞增殖活性，并与 PHA-767491 (HY-13461) 具有协同作用，使其抗增殖活性被进一步放大[1]。

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

AurkA allosteric-IN-1 相关抗体:

Cell Cycle Analysis[1]

Cell Line: HeLa and Panc-1 cells, Lung cancer cell lines (A549 and H358), and colon cancer cell lines (HT29 and HCT116)
Concentration: 20 μM
Incubation Time: 12, 24, and 48 h
Result: Arrested cell cycle at G1/S transition in lung cancer cell lines (A549 and H358), and arrested cell cycle at G2/M in colon cancer cell lines (HT29 and HCT116).
Almostly unaffected HeLa and Panc-1 cells.

Western Blot Analysis[1]

Cell Line: HT29 and HCT116 cells
Concentration: 20 μM
Incubation Time: 48 h
Result: Sharply downregulated the level of phospho-histone H3 (Ser10).

Cell Cytotoxicity Assay[1]

Cell Line: HeLa cells
Concentration: 25 μM, 50 μM, 100 μM, 200 μM, and 400 μM
Incubation Time: 12, 24, and 48 h; with or without PHA-767491
Result: With PHA-767491 sensitized HeLa cells, significantly augmented anti-proliferative activity GI50: 71.7 μM to GI50: 14.0 μM by co-treatment of 1.5 μM PHA-76749.
分子量

332.35

Formula

C20H16N2O3
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

AurkA allosteric-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)

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.

Keywords:

AurkA allosteric-IN-1Aurora KinaseAllosteric inhibitorAurkAAurora kinaseTPX2Inhibitorinhibitorinhibit

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