Cell Cycle/Checkpoint PLK BI 2536

BI 2536

Catalog No. T6173   CAS 755038-02-9

BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.

BI 2536, CAS 755038-02-9
Pack Size Availability Price/USD Quantity
2 mg In stock 87.00
5 mg In stock 123.00
10 mg In stock 219.00
25 mg In stock 359.00
50 mg In stock 575.00
100 mg In stock 929.00
1 mL * 10 mM (in DMSO) In stock 140.00
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Description BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
Targets&IC50 Met : ic50 4.754μM,   PI3Kα : ic50 2.407μM,   PLK1 : ic50 0.83nM,   PLK2 : ic50 3.5nM,   PLK3 : ic50 9.0nM,  
In vitro BI 2536 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 [1]. On treatment with nanomolar doses of BI 2536, ATC cells progressed normally through S phase but died thereafter, directly from mitotic arrest. Nontransformed thyroid cells were 3.2- to 18.4-fold less susceptible to BI 2536-induced cell cycle effects compared with ATC cells [2].
In vivo 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 [1].
Kinase Assay Plk1 in vitro kinase assay: Recombinant human Plk1 (residues 1-603) is expressed as N-terminal, GST-tagged fusion protein with a baculoviral expression system and purified by affinity chromatography with Glutathione-agarose. Enzyme activity assays for Plk1 are performed in the presence of serially diluted BI 2536 with 20 ng of recombinant kinase and 10 μg casein from bovine milk as the substrate. Kinase reactions are performed in a final volume of 60 μL for 45 minutes at 30 °C (15 mM MgCl2, 25 mM MOPS [pH 7.0], 1 mM DTT, 1% DMSO, 7.5 mM ATP, 0.3 μCi γ-33P-ATP). Reactions are terminated by the addition of 125 μL of ice-cold 5% TCA. After transfer of the precipitates to Multi-Screen mixed ester cellulose filter plates, plates are washed with 1% TCA and quantified radiometrically. Dose-response curve is used for calculating IC50 value.
Cell Research
Cells are exposed to various concentrations of BI 2536 for 24, and 72 hours. Cell growth is assessed by the measurement of Alamar Blue dye conversion in a fluorescence spectrophotometer. For determining the DNA content of the cultures, cell suspensions are fixed in 80% ethanol, treated for 5 minutes with 0.25% Triton X-100 in PBS, and incubated with 0.1% RNase and 10 μg/mL propidium iodide (PI) in PBS for 20 minutes at RT. Cell-cycle profiles are determined by flow cytometric analysis.(Only for Reference)
Cell lines: HeLa, A43, SKOV-3, HT-29, K562, A549, Saos-2, MCF7, HCT116, COLO 205, Hep G2, Raji and PC-3 cells, etc.
Animal Research
Animal Model: FeBomTac:NMRI-Foxn1nu mice injected subcutaneously with HCT 116, NCI-H460, or A549 cells
Molecular Weight 521.66
Formula C28H39N7O3
CAS No. 755038-02-9


0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 20 mg/mL (38.3 mM)

Ethanol: 93 mg/mL (178.3 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 15 mg/mL


References and Literature
1. Steegmaier M, et al. BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo. Current Biology (2007), 17(4), 316-322. 2. Nappi TC, et al. Identification of Polo-like kinase 1 as a potential therapeutic target in anaplastic thyroid carcinoma. Cancer Res. 2009 Mar 1;69(5):1916-23. 3. Chen L, et al. BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. ACS Med Chem Lett. 2015 May 18;6(7):764-9. 4. Malik N, et al. Suppression of IFN β gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members. Biochem J. 2015 Jun 15;468(3):363-72.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Epigenetics Compound Library PI3K-AKT-mTOR Compound Library Tyrosine kinase inhibitor library DNA Damage & Repair Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Histone Modification Research Compound Library Cell cycle related Compound Library

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