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

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
1 mg USD 44 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
200 mg   Get quote  
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 42 publication(s) in Google Scholar

BI 2536 Related Antibodies

Top Publications Citing Use of Products

39 Publications Citing Use of MCE BI 2536

WB

    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.

    View All Polo-like Kinase (PLK) Isoform Specific Products:

    View All Isoforms
    PLK1 PLK2 PLK3 PLK4

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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]

    PLK1

    0.83 nM (IC50)

    Plk2/Snk

    3.5 nM (IC50)

    Plk3/Fnk

    9 nM (IC50)

    BRD4

    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.

    BI 2536 Related Antibodies
    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

    521.65

    Formula

    C28H39N7O3
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C1[C@H](N(C2=C(N1C)C=NC(NC3=CC=C(C(NC4CCN(C)CC4)=O)C=C3OC)=N2)C5CCCC5)CC
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 65 mg/mL (124.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

    Preparing
    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      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

      This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      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

      This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.95%

    COA (251 KB) HNMR (213 KB) LCMS (465 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [3]

    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
    [3]

    Mice[3]
    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.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    0.1 M HCL / DMSO 1 mM 1.9170 mL 9.5850 mL 19.1699 mL 47.9249 mL
    5 mM 0.3834 mL 1.9170 mL 3.8340 mL 9.5850 mL
    10 mM 0.1917 mL 0.9585 mL 1.9170 mL 4.7925 mL
    15 mM 0.1278 mL 0.6390 mL 1.2780 mL 3.1950 mL
    20 mM 0.0958 mL 0.4792 mL 0.9585 mL 2.3962 mL
    25 mM 0.0767 mL 0.3834 mL 0.7668 mL 1.9170 mL
    30 mM 0.0639 mL 0.3195 mL 0.6390 mL 1.5975 mL
    40 mM 0.0479 mL 0.2396 mL 0.4792 mL 1.1981 mL
    DMSO 50 mM 0.0383 mL 0.1917 mL 0.3834 mL 0.9585 mL
    60 mM 0.0319 mL 0.1597 mL 0.3195 mL 0.7987 mL
    80 mM 0.0240 mL 0.1198 mL 0.2396 mL 0.5991 mL
    100 mM 0.0192 mL 0.0958 mL 0.1917 mL 0.4792 mL
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    BI 2536 Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    BI 2536755038-02-9BI2536BI-2536Polo-like Kinase (PLK)Epigenetic Reader DomainApoptosisInhibitorinhibitorinhibit

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