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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.

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BI 2536, CAS 755038-02-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 105.00
25 mg	In stock	$ 126.00
50 mg	In stock	$ 207.00
100 mg	In stock	$ 369.00
500 mg	In stock	$ 885.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 98.31%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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	PLK3:9 nM (cell free), PLK1:0.83 nM (cell free), PLK2:3.5 nM (cell free)
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	Recombinant human Plk1 (residues 1–603) was 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, Plk2, and Plk3 were performed in the presence of serially diluted inhibitor with 20 ng of recombinant kinase and 10 μg casein from bovine milk as the substrate. Kinase reactions were performed in a final volume of 60 μl for 45 min at 30C (15 mM MgCl2, 25 mM MOPS [pH 7.0], 1 mM DTT, 1% DMSO, 7.5 μM ATP, 0.3 μCi g-P33-ATP). Reactions were terminated by the addition of 125 μl of ice-cold 5% TCA. After transfer of the precipitates to MultiScreen mixed ester cellulose filter plates, plates were washed with 1% TCA and quantified radiometrically. Dose-response curves were used for calculating IC50 values [1].
Cell Research	Cell proliferation assays were performed by incubation in the presence of various concentrations of BI 2536 for 72 hr, and cell growth was assessed by the measurement of Alamar Blue dye conversion in a fluorescence spectrophotometer. Effective concentrations at which cellular growth was inhibited by 50% (EC50) were extrapolated from the dose-response curve fit [1].
Animal Research	Female BomTac:NMRI-Foxn1nu mice were grafted subcutaneously with HCT 116 colon-carcinoma, NCI-H460, or A549 lung carcinoma cells by subcutaneous injection, respectively, of 2 × 10^6, 1 × 10^6, and 1 × 10^7 cells into the flank of each mouse. When tumors reached a volume of approximately 50 mm^3, animals were pair-matched into treatment and control groups of ten mice each. In regression experiments, treatment was not initiated until the mean tumor volume reached 500 mm^3. BI 2536 was formulated in hydrochloric acid (0.1 N), diluted with 0.9% NaCl, and injected intravenously into the tail vein at the indicated dose and schedule. The administration volume was 10 ml per kg body weight. Tumor volumes were determined three times a week with a caliper. The results were converted to tumor volume (mm^3) by the following formula: length × width2 × π/6. The weight of the mice was determined as an indicator of tolerability on the same days. For statistical analysis, the treatment group was compared with the vehicle control group in a one-sided (decreasing) exact Wilcoxon test [1].

Molecular Weight	521.65
Formula	C28H39N7O3
CAS No.	755038-02-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 93 mg/mL (178.3 mM)

DMSO: 20 mg/mL (38.3 mM)

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. Guo C, Zhu J, Wang J, et al. Neuroprotective effects of protocatechuic aldehyde through PLK2 /p-GSK3β/Nrf2 signaling pathway in both in vivo and in vitro models of Parkinson's disease. Aging-us. 2019, 11. 4. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent[J]. Scientific reports. 2018 Oct 8;8(1):14969.

Citations

1. Zhang Y, Hong X, Hua S, et al. Reconstitution and mechanistic dissection of the human microtubule branching machinery. Journal of Cell Biology. 2022, 221(7): e202109053 2. Guo C, Zhu J, Wang J, et al. Neuroprotective effects of protocatechuic aldehyde through PLK2 /p-GSK3β/Nrf2 signaling pathway in both in vivo and in vitro models of Parkinson's disease. Aging-us. 2019, 11 3. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. Scientific Reports. 2018 Oct 8;8(1):14969 4. Wang D, Wang Y, Di X, et al.Cortical tension drug screen links mitotic spindle integrity to Rho pathway.Current Biology.2023 5. Kong Y, Liu Y, Li X, et al.Palmitoylation landscapes across human cancers reveal a role of palmitoylation in tumorigenesis.Journal of Translational Medicine.2023, 21(1): 1-19.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Inhibitor Library Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Drug Repurposing Compound Library PPI Inhibitor Library Anti-Aging Compound Library ReFRAME Related Library

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Keywords

BI 2536 755038-02-9 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Epigenetic Reader Domain PLK BI-2536 Inhibitor BI2536 inhibit Polo-like Kinase (PLK) inhibitor

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