Current biology : CBFeb 13, 2007

BI 2536, a strong and selective blocker of a key cell division enzyme, slows tumor growth in living organisms

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Updated Apr 4, 2026

Abstract

The small-molecule inhibitor BI 2536 inhibits Plk1 enzyme activity at low nanomolar concentrations.

BI 2536 causes mitotic arrest and induces apoptosis in diverse human cancer cell lines.
In vivo studies show BI 2536 inhibits growth of human tumor xenografts in nude mice.
Treatment with BI 2536 leads to tumors arresting in prometaphase and accumulating phosphohistone H3.
Aberrant mitotic spindles are observed in tumor cells treated with BI 2536.
A surge in apoptosis is detectable through immunohistochemistry and imaging techniques.

Simplified

Fine-mapping of the cell-division cycle, notably the identification of mitotic kinase signaling pathways, provides novel opportunities for cancer-drug discovery. As a key regulator of multiple steps during mitotic progression across eukaryotic species, the serine/threonine-specific Polo-like kinase 1 (Plk1) is highly expressed in malignant cells and serves as a negative prognostic marker in specific human cancer types . Here, we report the discovery of a potent small-molecule inhibitor of mammalian Plk1, BI 2536, which inhibits Plk1 enzyme activity at low nanomolar concentrations. The compound potently causes a mitotic arrest and induces apoptosis in human cancer cell lines of diverse tissue origin and oncogenome signature. BI 2536 inhibits growth of human tumor xenografts in nude mice and induces regression of large tumors with well-tolerated intravenous dose regimens. In treated tumors, cells arrest in prometaphase, accumulate phosphohistone H3, and contain aberrant mitotic spindles. This mitotic arrest is followed by a surge in apoptosis, detectable by immunohistochemistry and noninvasive optical and magnetic resonance imaging. For addressing the therapeutic potential of Plk1 inhibition, BI 2536 has progressed into clinical studies in patients with locally advanced or metastatic cancers.

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BI 2536, a strong and selective blocker of a key cell division enzyme, slows tumor growth in living organisms

Abstract

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