AURKA against 1
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.
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- Formule: C28H32FN9O2
- Masse moléculaire:545.61
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
In Vitro
Ac13 (0-10 μM, 3 h) inhibits tumor proliferation, with GI50 of 588, 86 and 6.6 nM in K562, HL-60, and CCRF-CEM cells, inhibiting AURKA autophosphorylation and cell viability in a dose-dependent manner[1].
Ac13 (10 μM, 1 h)-induced K162 acetylation of endogenous AURKA is reversible in HCT116 cells expressing SIRT3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562
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Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM; 2 μM
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Incubation Time:3 h for 0-10 μM; 2 μM for 1h
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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).
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Cell Line:HCT116 and HCT116 successfully expressed SIRT3
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Concentration:10 μM
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Incubation Time:1h
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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.
Chemical Information
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Masse moléculaire 545.61
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Formule C28H32FN9O2
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SMILES
CC(OC1=CC(CNC2=CC=C(NC3=NC(N4CCN(C)CC4)=CC(NC5=NNC(C)=C5)=N3)C=C2)=CC=C1F)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AURKA against 1 Related Classifications
HY-162837 Related Classifications
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