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ZM 447439 - 5mg

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Cell Cycle/Checkpoint : Aurora Kinase , Chromatin/Epigenetics : Aurora Kinase , store at -20°C
 
Aurora Kinase Inhibitor is a potent and selective small molecule inhibitor primarily known for its ability to inhibit the Aurora B kinase, a key protein in cell division. Aurora B kinase is part of the chromosomal passenger complex and plays a crucial role in regulating mitosis.

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Molecular Properties:

  • Chemical Structure: ZM 447439 is a synthetic small molecule designed to selectively inhibit Aurora B kinase. It is part of the broader class of Aurora kinase inhibitors, which target the function of these enzymes in mitosis. Its structure enables it to bind specifically to the ATP-binding pocket of Aurora B, preventing its activation and subsequent mitotic processes.
  • Mechanism of Action: ZM 447439 works by inhibiting Aurora B kinase activity. Aurora B is a central player in the mitotic process, particularly in chromosome alignment, spindle assembly checkpoint regulation, and cytokinesis. By inhibiting Aurora B, ZM 447439 prevents proper chromosome segregation, leading to mitotic arrest and, eventually, apoptosis (programmed cell death).
  • Selectivity: ZM 447439 is highly selective for Aurora B over other Aurora kinases (like Aurora A and Aurora C) and kinases in general. This specificity is crucial because it minimizes off-target effects, allowing researchers to study the precise role of Aurora B kinase without interference from other kinases in the cell.
  • Cellular Target: Aurora B kinase regulates chromosome attachment to spindle microtubules and is integral to the mitotic checkpoint. ZM 447439 inhibits this kinase and induces mitotic defects by preventing the proper alignment and segregation of chromosomes. This leads to a halt in cell division and often triggers cell death via apoptosis.

Key Advantages:

  • Specificity for Aurora B Kinase: ZM 447439’s high selectivity for Aurora B allows precise targeting of this kinase without broad interference from other kinases.
  • Induces Mitotic Arrest and Apoptosis: ZM 447439 is effective in inducing mitotic defects and apoptosis in cancer cells, making it an important tool in cancer research.
  • Potential for Combination Therapies: Its use in combination with other therapeutic agents can improve treatment outcomes for cancers with high mitotic activity.
  • Insights into Chromosomal Instability: ZM 447439 aids in studying the consequences of chromosomal instability, which is a hallmark of many cancers.

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