1. PROTAC Epigenetics Cell Cycle/DNA Damage Neuronal Signaling Cytoskeleton Protein Tyrosine Kinase/RTK
  2. PROTACs Aurora Kinase AAK1 Cyclin G-associated Kinase (GAK) Mps1 FAK
  3. dAurAB5

dAurAB5 是一种双重 Aurora-A (DC50 = 8.8 nM) 和 Aurora-B (DC50 = 6.1 nM) PROTAC 降解剂。dAurAB5 诱导 Aurora-AAurora-B 降解,降低 N-Myc 水平并降低 IMR32 神经母细胞瘤细胞的活力。dAurAB5 下调 AAK1、PTK2、GAK、TTK 的水平。dAurAB5 可用于研究神经母细胞瘤等癌症。(粉色:TTK ligand 2:HY-168542,蓝色:Thalidomide-O-COOH:HY-103597,黑色:6-Aminocaproic acid:HY-B0236)。

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dAurAB5

dAurAB5 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

dAurAB5 is a dual Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma. (Pink: TTK ligand 2: HY-168542, Blue: Thalidomide-O-COOH: HY-103597, Black: 6-Aminocaproic acid: HY-B0236)[1].

IC50 & Target[1]

Cereblon

 

Aurora-A

8.8 nM (DC50)

Aurora-B

6.1 nM ()

体外研究
(In Vitro)

dAurAB5 (500 nM,24 小时) 可诱导 Aurora-A 和 Aurora-B 显著降解,降解率分别为 84% 和 82%[1]
dAurAB5 (500 nM,24 小时) 可使 IMR32 细胞中的 N-Myc 水平降低 45%[1]
dAurAB5 (100 nM,4 小时) 可使 IMR32 细胞中的 Aurora-A 降解 83%,Aurora-B 降解 95%[1]
dAurAB5 (200 nM,6 小时) 在 MYCN 扩增的 Kelly 神经母细胞瘤细胞中可降低 Aurora-A 的丰度以及 AAK1、PTK2、GAK、TTK 的水平,但不会下调的 Aurora-B 丰度[1]
dAurAB5 (0-1000 nM,24 小时) 可降低 IMR32 细胞的细胞活力,但对 HEK293 细胞的细胞毒性极小[1]

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

Western Blot Analysis[1]

Cell Line: IMR32 cells
Concentration: 500 nM
Incubation Time: 24 h
Result: Reduced N-Myc levels by 45%.

Western Blot Analysis[1]

Cell Line: IMR32 cells
Concentration: 100 nM
Incubation Time: 4 h
Result: Degraded 83% of Aurora-A and 95% of Aurora-B.

Cell Viability Assay[1]

Cell Line: IMR32 cells
Concentration: 0, 10, 100, 1000 nM
Incubation Time: 24 h
Result: Significant reduced cell viability, with 45% reduction in cell viability at 100 nM and 55% reduction in cell viability at 1 μM.
分子量

819.91

Formula

C42H49N11O7

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:
dAurAB5
目录号:
HY-171770
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