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Enzymes for Research, Diagnostic and Industrial Use

BI 2536

Cat No.
CEI-0295
Description
BI 2536 can inhibit PLK1 with IC50 of 0.83 nM.
CAS No.
755038-02-9
Molecular Weight
521.66
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
PLK1
Molecular Formula
C28H39N7O3
Chemical Name
(R)-4-(8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylamino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
Solubility
DMSO 96 mg/mL Water
In vitro
BI 2536 is a potent and selective inhibitor of Plk1 (Polo-like kinase 1), while Polo-like kinase 1 is characterized extensively to further understanding of mitotic mechanisms and as potential targets for cancer therapy. BI 2536 blocks Plk1 activity fully and instantaneously. BI 2536 inhibited primary human cells (HUVEC) with IC50 of 30 nM. And BI 2536 blocked the cancer cell line HeLa with IC50 of 9 nM. Cells treated with BI 2536 are delayed in prophase but eventually import Cdk1-cyclin B into the nucleus, enter prometaphase, and degrade cyclin A. BI 2536-treated cells lack prophase microtubule asters and thus polymerize mitotic microtubules only after nuclear-envelope breakdown and form monopolar spindles that do not stably attach to kinetochores. BI 2536 potently caused a mitotic arrest and induced apoptosis in human cancer cell lines of diverse tissue origin and oncogenome signature. (1) Chronic myeloid leukemia (CML) BI 2536 can inhibit proliferation of imatinib-sensitive and imatinib-resistant CML cells. BI 2536 inhibited leukemic cells, which carries the T315 mutation of BCR/ABL with IC50 values from 1nM to 50 nM. The growth-inhibitory effects of BI 2536 on CML cells were found to be associated with cell cycle arrest and apoptosis. BI 2536 also synergized with imatinib and nilotinib in producing growth inhibition in CML cells. (2) Cardiac fibroblasts BI 2536 had a profound effect on cardiac fibroblast proliferation in vitro and arrested these cells in mitosis with an IC50 of about 43 nM.
In vivo
BI 2536 inhibited growth of human tumor xenografts in nude mice and induces regression of large tumors.
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