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 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).

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dAurAB5

dAurAB5 Chemical Structure

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Description

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 ()

In Vitro

dAurAB5 (500 nM, 24 h) induces significant degradation of Aurora-A and Aurora-B, with degradation rates of 84% and 82%[1].
dAurAB5 (500 nM, 24 h) reduces N-Myc levels by 45% in IMR32 cells[1].
dAurAB5 (100 nM, 4 h) degrades 83% of Aurora-A and 95% of Aurora-B in IMR32 cells[1].
dAurAB5 (200 nM, 6 h) decreases the abundance Aurora-A and the levels of AAK1, PTK2, GAK, TTK, but does not downregulated Aurora-B abundance in the MYCN-amplified Kelly neuroblastoma cells[1].
dAurAB5 (0-1000 nM, 24 h) reduces cell viability in IMR32 cells, but has minimal cytotoxicity in HEK293 cells[1].

MedChemExpress (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.
Molecular Weight

819.91

Formula

C42H49N11O7

SMILES

O=C(NCCCCCC(N1CCN(C2=CC=C(NC3=NC(NC4CCCCC4)=C5N=CNC5=N3)C=C2)CC1)=O)COC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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dAurAB5
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HY-171770
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