Chemicals of Shanghai APIs Chemical Co.,
Boehringer PLK-1 inhibitor
|CAS Registry Number:
Storage: 4 deg.
For Research Use Only
Biological Activity of BI 2536:
BI 2536 is a small molecule compound with
potential antineoplastic activities. BI 2536
binds to and inhibits Polo-like kinase 1 (Plk1,
derived from human, mouse and rat) (with IC50of
0.83 nM), resulting in mitotic arrest,
disruption of cytokinesis, and apoptosis in
susceptible tumor cell populations. Plk1, a
serine/threonine-protein kinase, is a key
regulator of multiple processes fundamental to
mitosis and cell division.
This compound showed a more than 1000-fold
selectivity relative to a panel of 63 other
protein kinases, but it also affected the
activities of Plk2 at an IC50 of 3.5 nM and, to
a slightly lesser extent, the activity of Plk3
(IC50 9.0 nM).
The half-maximal effective concentration (EC50)
values in a panel of 32 human cancer cell lines
ranged 2–25 nM.
BI 2536 inhibits growth of human tumor
xenografts in nude mice and induces regression
of large tumors with well-tolerated intravenous