dnAurA-A10
dnAurA-A10 is a potent and selective AURKA PROTAC degrader. dnAurA-A10 recruits the L3MBTL3-DCAF5 E3 ubiquitin ligase complex, which is primarily localized in the nucleus, thereby achieving spatially specific ubiquitination and proteasomal degradation of AURKA protein in the nucleus. dnAurA-A10 can be used for research on colorectal cancer.
(Pink: Aurora A ligand (HY-10971); Blue: DCAF5 ligand (HY-188402); Black: linker (HY-W016871)).
For research use only. We do not sell to patients.
- Formula: C70H83ClFN11O6
- Molecular Weight:1228.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
Aurora A |
DCAF5 |
In Vitro
dnAurA-A10 (70-633 nM; 20 h) stabilizes or slightly increases nuclear AURKA fluorescence signal below the degradation threshold in HCT116-NLS-mNeonGreen-AURKA cells[1].
dnAurA-A10 (17-50 μM; 6-19.5 h) has an effect in HCT116-NLS-mNeonGreen-AURKA cells in which degradation efficiency decreases due to the "hook effect"[1].
dnAurA-A10 (10-50 μM; 24 h) selectively degrades nuclear AURKA protein in HCT116 cells (stably expressing exogenous or endogenous AURKA), with little effect on cytoplasmic AURKA[1].
dnAurA-A10 (72 h) significantly inhibits cell proliferation in HCT116 cells (with high nuclear AURKA expression) (IC50 = 3.24 μM); it shows almost no inhibitory effect on proliferation in MCF-10A cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 (and its stable cell lines HCT116-NLS-V5-AURKA, HCT116-AURKA-3xFLAG-NES)
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Concentration:0.0032, 0.016, 0.08, 0.4, 2, 5, 10, 25, 40, 50 μM
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Incubation Time:24 h
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Result:Induced specific degradation of nuclear AURKA at 10-50 μM (reducing levels to 30-40% in the nucleus), while causing only a modest reduction or even a compensatory upregulation of cytoplasmic AURKA.
Did not induce the degradation of AURKB.
Chemical Information
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Molecular Weight 1228.93
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Formula C70H83ClFN11O6
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SMILES
O=C(C1=CC=C(NC2=NC=C3C(C4=CC=C(Cl)C=C4C(C5=C(F)C=CC=C5OC)=NC3)=N2)C=C1OC)NCCCCCCCCCCNC(C6=CC=C(NC7=CC(C(N8CCC(N9CCCC9)CC8)=O)=CC=C7C(N%10CCC(N%11CCCC%11)CC%10)=O)C=C6)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
dnAurA-A10 Related Classifications
HY-188401 Related Classifications
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