Aurora Kinase Inhibitor XI, HOI-07

Aurora Kinase Inhibitor XI, HOI-07
(E)-3-((E)-4-(Benzo[d][1,3]dioxol-5-yl)-2-oxobut-3-enylidene)indolin-2-one
A cell-permeable oxindole compound that selectively inhibits Aurora B, but not Aurora A, activity (IC50 ≤100 nM; [ATP] = 100 µM) and potently suppresses cellular histone H3 Ser10 phosphorylation (IC50 <100 nM in A549 cells; 24 h) by targeting kinase ATP-binding site, exhibiting much reduced potency toward a panel of 49 other kinases (≤53% inhibition at 5 µM). Although noncytotoxic at ≤1 µM, HOI-07 treatment does induce G2/M arrest and apoptosis in A549 culutres at higher concentrations (5 µM). Potently inhibits anchorage-independent growths of human lung and colon cancer lines (by >80% at 0.5 µM) in vitro and is efficacious in suppressing A549 tumor expansion in mice (10, and 20 mg/kg; twice weekly i.p.) in vivo.
产品信息
Form  Red solid
Primary Target  Aurora B
Molar mass  319.3
Protect from Light  是的
Packaged under inert gas  是的
Cell permeable  是的
Reversible  是的
Purity  ≥97% by HPLC
Solubility  DMSO
商店和运输信息
Storage  +2°C to +8°C
Ship  Ambient Temperature Only
Standard Handling