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

AURKA against 1 Chemical Structure

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AURKA against 1 Related Antibodies

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Description

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].

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.

AURKA against 1 Related Antibodies

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.
Molecular Weight

545.61

Formula

C28H32FN9O2
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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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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AURKA against 1 Related Classifications

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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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