2. Cell Cycle/DNA Damage Epigenetics
  3. Aurora Kinase
  4. AURKA against 1

AURKA against 1(compound Ac13) 是 Aurora 激酶 (AURKA) 的抑制剂 (IC50 小于 0.5 nM)，靶向内源性赖氨酸 (K162) 乙酰化，并具有抗肿瘤细胞增殖活性。AURKA against 1 诱导的 K162 乙酰化的 AURKA 的激酶活性在转染 SIRT3 的 HCT116 细胞中被可逆的恢复。

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AURKA against 1 Chemical Structure

AURKA against 1 Chemical Structure

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AURKA against 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AURKA against 1 is an inhibitor of AURKA (IC50 less than 0.5 nM), targeting endogenous lysine (K162) acetylation, and has anti-proliferation activity against tumor cells. AURKA against 1 induces K162 acetylation, and the kinase activity of AURKA is reversibly restored in HCT116 cells transfected with SIRT3[1].

体外研究
(In Vitro)

Ac13 (0-10 μM，3 h) 抗肿瘤增殖，在 K562，HL-60，CCRF-CEM 细胞中 GI50 为 588，86，6.6 nM，以剂量依赖的方式抑制 AURKA 的自磷酸化，抑制细胞活性[1]。
Ac13 (10 μM，1 h) 诱导的内源性 AURKA 的 K162 乙酰化在表达 SIRT3 的 HCT116 细胞中是可逆的[1]。

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

AURKA against 1 相关抗体:

Western Blot Analysis[1]

Cell Line: K562
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM; 2 μM
Incubation Time: 3 h for 0-10 μM; 2 μM for 1h
Result: Inhibited endogenous autophosphorylation of AURKA (T288) in a dose-dependent manner at 0-10 μM. K562 cell viability and AURKA autophosphorylation could be continuously inhibited after washout test.
Induced potent acetylation of endogenous AURKA, and endogenous AURKA acetylated at K162 in K562 cells treated with Ac13 (2 μM, 1 h) was blocked by X1 (covalently modifiable lysine) (20 μM, 1 h). Ac13 (20 μM, 1 h) effectively blocked XO44 (covalently modifiable lysine) labeling of K562/HL-60 cells and could maintain the selectivity of VX-680 (a noncovalent inhibitor of AURKA).

Cell Cytotoxicity Assay[1]

Cell Line: HCT116 and HCT116 successfully expressed SIRT3
Concentration: 10 μM
Incubation Time: 1h
Result: Induced acetylation of AURKA in HCT116 cells, inhibited endogenous AURKA activity and p53 degradation.
Abolished AURKA and restored the kinase activity of K162-acetylated AURKA as well as p53 phosphorylation and degradation after successful expression of SIRT3.
分子量

545.61

Formula

C28H32FN9O2
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 against 1 相关分类

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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:

AURKA against 1AURKA against1AURKA against-1Aurora KinaseAURKAAcetylationReversible InhibitionSIRT3HCT116Inhibitorinhibitorinhibit

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AURKA against 1
目录号：
HY-162837
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