1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. Polo-like Kinase (PLK) Epigenetic Reader Domain Apoptosis
  3. BI 2536

BI 2536 

Cat. No.: HY-50698 Purity: 99.76%
COA Handling Instructions

BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription.

For research use only. We do not sell to patients.

BI 2536 Chemical Structure

BI 2536 Chemical Structure

CAS No. : 755038-02-9

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 126 In-stock
10 mM * 1 mL in DMSO USD 126 In-stock
5 mg USD 110 In-stock
10 mg USD 165 In-stock
50 mg USD 275 In-stock
100 mg USD 495 In-stock
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500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 37 publication(s) in Google Scholar

Top Publications Citing Use of Products

34 Publications Citing Use of MCE BI 2536


    BI 2536 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Apr;17(4):825-837.  [Abstract]

    Effect of Plk1 inhibitor on cell proliferation of TAMR-MCF-7 cells. Effects of BI2536 on Plk1 signaling in TAMR-MCF-7 cells. TAMR-MCF-7 cells are incubated with BI2536 (1, 5 and 10 nM) for 24 h and total cell lysates are subjected to immunoblottings for Plk1, Cdc25c and Cyclin B1.

    BI 2536 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Nov 22;8(1):1701.  [Abstract]

    Cells are transfected and treated with BI 2536 as indicated and were fractionated into cytoplasmic (C) and nuclear (N) fractions analyzed by Western blots. The position of Cdc25 and its phosphorylated forms are indicated by arrows. MEK and Histone H3 are respectively cytoplasmic and nuclear proteins probed as controls.

    BI 2536 purchased from MedChemExpress. Usage Cited in: College of Pharmacy. Seoul National University. 2015 Feb.

    Plk1 inhibition-mediated down-regulation of cdc25c and up-regulation of cyclin B1 in TAMR-MCF-7. BI 2536 (1, 5 and 10 nM) is treated for either 24 h or 48 h.

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    • Biological Activity

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    • Customer Review


    BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively[1]. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription[4].

    IC50 & Target[1]


    0.83 nM (IC50)


    3.5 nM (IC50)


    9 nM (IC50)


    25 nM (IC50)

    In Vitro

    Exceeding a 100-fold concentration range starting at 10 nM, BI 2536 causes HeLa cells to accumulate with a 4N DNA content, indicative of a cell-cycle block in either G2 phase or mitosis. In addition to HeLa cells, BI 2536 potently inhibits the proliferation of a panel of 32 human cancer cell lines, representing diverse organ derivations (including carcinomas of the breast, colon, lung, pancreas, and prostate, melanomas, and hematopoietic cancers) and varied patterns of tumor suppressor or oncogene mutations (including RB1, TP53, PTEN, andKRAS status). The half-maximal effective concentration (EC50) values in this cell panel ranged 2-25 nM, whereas a concentration of 100 nM of BI 2536 is typically sufficient for inducing a complete mitotic arrest. The proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells is blocked at EC50values ranging 12-31 nM, indicating a comparable sensitivity of cycling nontransformed cells to BI 2536[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    BI 2536 (40-50 mg/kg, i.v.) blocks the growth of human cancer xenografts in immunodeficient, nu/nu mice. Consecutive cycles of 40-50 mg/kg BI 2536 given i.v. once or twice per week are found to be highly efficacious in diverse xenograft models, such as the HCT 116 colon cancer with complete tumor suppression with the twice per week schedule (treated versus the control (T/C) value 0.3%) and a T/C value of 16% with once per week treatment; both schedules are well-tolerated, as judged by clinical signs and absence of major body-weight changes[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight




    CAS No.



    White to light yellow




    Room temperature in continental US; may vary elsewhere.


    4°C, protect from light

    *In solvent : -80°C, 1 years; -20°C, 6 months (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 65 mg/mL (124.60 mM; Need ultrasonic)

    0.1 M HCL : 25 mg/mL (47.92 mM; ultrasonic and adjust pH to 4 with HCl)

    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9170 mL 9.5850 mL 19.1699 mL
    5 mM 0.3834 mL 1.9170 mL 3.8340 mL
    10 mM 0.1917 mL 0.9585 mL 1.9170 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 25 mg/mL (47.92 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 3.25 mg/mL (6.23 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 3.25 mg/mL (6.23 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.99 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.95%

    Cell Assay

    Cell proliferation assays are performed by incubation in the presence of various concentrations of BI 2536 (10 nM-1 μM) for 72 hr, and cell growth is assessed by the measurement of Alamar Blue dye conversion in a fluorescence spectrophotometer. Effective concentrations at which cellular growth is inhibited by 50% (EC50) are extrapolated from the dose-response curve fit[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration

    Female BomTac:NMRI-Foxn1nu mice are grafted subcutaneously with HCT 116 colon-carcinoma, NCI-H460, or A549 lung-carcinoma cells by subcutaneous injection, respectively, of 2×106, 1×106, and 1×107 cells into the flank of each mouse. When tumors reached a volume of approximately 50 mm3, animals are pair-matched into treatment and control groups of ten mice each. In regression experiments, treatment is not initiated until the mean tumor volume reached 500 mm3. BI 2536 is injected intravenously into the tail vein at the indicated dose and schedule. The administration volume is 10 mL per kg body weight. Tumor volumes are determined three times a week with a caliper. The results are converted to tumor volume (mm3) by the following formula: length×width2×π/6. The weight of the mice is determined as an indicator of tolerability on the same days. For statistical analysis, the treatment group is compared with the vehicle control group in a one-sided (decreasing) exact Wilcoxon test.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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