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Compound Ac13, also termed AURKA against 1, acts as an inhibitor of the Aurora kinase (AURKA) with an IC50 of less than 0.5 nM, targeting the acetylation of endogenous lysine (K162) and exhibiting anti-tumor cell proliferation activity. The kinase activity of AURKA, acetylated at K162 and induced by AURKA against 1, is reversibly restored in HCT116 cells transfected with SIRT3.
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Description | Compound Ac13, also termed AURKA against 1, acts as an inhibitor of the Aurora kinase (AURKA) with an IC50 of less than 0.5 nM, targeting the acetylation of endogenous lysine (K162) and exhibiting anti-tumor cell proliferation activity. The kinase activity of AURKA, acetylated at K162 and induced by AURKA against 1, is reversibly restored in HCT116 cells transfected with SIRT3. |
In vitro | Ac13 (0-10 μM, 3 h) exhibits antitumor proliferation effects, displaying GI50 values of 588 nM, 86 nM, and 6.6 nM in K562, HL-60, and CCRF-CEM cells, respectively. It inhibits AURKA autophosphorylation in a dose-dependent manner and suppresses cell viability. Moreover, Ac13 (10 μM, 1 h) induces reversible acetylation of endogenous AURKA at K162 in HCT116 cells expressing SIRT3. |
Molecular Weight | 545.61 |
Formula | C28H32FN9O2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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