2. Cell Cycle/DNA Damage
  3. CDK
  4. BI-1347

BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity.

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

The BI-1347 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

CAS No. : 2163056-91-3

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Customer Review

Based on 6 publication(s) in Google Scholar

BI-1347 Related Antibodies

Top Publications Citing Use of Products

    BI-1347 purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2025 Oct 16;18(10):1560.  [Abstract]

    CDK8 inhibitor (BI-1347 (0.0001-100 μM; 4 days) were assessed for their level of cytotoxicity by a Neutral Red uptake assay (orange) and their antiviral activity (black) on COS-7 cells.

    BI-1347 purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2025 Oct 16;18(10):1560.  [Abstract]

    Summarized results for different cell types (Vero, COS-7 and HFFs) or different method approaches (GFP or qPCR) for the CDK8 inhibitors (BI-1347, CCT-251921, MSC-2530818) or reference compounds (BCV, CDV, GCV) based on the EC50, CC50, and SI of at least three replications; n.d. not determined.

    BI-1347 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 9.

    MCF10A cells were plated at equal low density and either mock treated or treated with 31 nM BI-1347, in the presence or absence of 1.25 µM or 10 µM XL413 over a 7-day period. Representative image of plates stained with crystal violet. The results showed that adding the CDK8 inhibitor BI-1347 to MCF10A cells only marginally inhibited their proliferation; in contrast, BI-1347 strongly reduced cell growth when BI-1347 was combined with either 1.25 µM or 10 µM of the CDC7i XL413.

    BI-1347 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 9.

    MCF10A cells were mock treated or treated for 24 hours with three different CDK8 inhibitors: 31 nM BI-1347, 5 µM Senexin A, or 100 nM CCT-251921, alone or in combination with either 10 µM XL413 or 0.3 µM TAK-931 CDC7 inhibitors. Cells were labelled with EdU for last 30 minutes and DNA synthesis, DNA content and cell cycle distribution were assessed by flow cytometry.

    BI-1347 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 9.

    MCF10A cells were either mock treated, treated with 31 nM BI-1347 alone, with 10 µM XL413 with or in combination of both or with 2mM Hydroxyurea (HU) for 24 hours. Whole cell extracts, or soluble and chromatin-enriched fractions were analysed by immunoblotting for the indicated proteins. TPS (total protein stain) is used as a loading control. Asterisks indicate non-specific bands.

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity[1][2].

    IC50 & Target[1]

    CDK8

    1.1 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    32.94 μM
    Compound: BI-1347
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
    		[PMID: 36930701]
    HEK293 EC50
    5 nM
    Compound: 28; BI-1347
    Inhibition of mouse derived homozygous Tg0N4R P301S mutant tau-induced human ON4R tau aggregation harboring P301S mutant transfected in HEK293 cells preincubated for 2 hrs followed by compound addition and measured after 3 hrs by YFP-based fluorescence assay
    Inhibition of mouse derived homozygous Tg0N4R P301S mutant tau-induced human ON4R tau aggregation harboring P301S mutant transfected in HEK293 cells preincubated for 2 hrs followed by compound addition and measured after 3 hrs by YFP-based fluorescence assay
    		[PMID: 32071678]
    MDA-MB-231 IC50
    28.65 μM
    Compound: BI-1347
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
    		[PMID: 36930701]
    MDA-MB-468 IC50
    28.82 μM
    Compound: BI-1347
    Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
    Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
    		[PMID: 36930701]
    In Vitro

    BI-1347 (150 nM; 44 h) enhances granzyme B (GZMB+) production in mouse splenic NK cells[2].
    BI-1347 (0.1 nM-10 μM; 24 h) treatment increases perforin secretion from NK92MI cells[2].

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

    BI-1347 Related Antibodies

    Western Blot Analysis[2]

    Cell Line: Mouse splenic NK cells
    Concentration: 150 nM
    Incubation Time: 44 hours
    Result: Increased the proportion of granzyme B-positive NK cells by approximately 4-fold.

    Western Blot Analysis[2]

    Cell Line: Human NK92MI cells
    Concentration: 0.1 nM-10 μM
    Incubation Time: 24 hours
    Result: Increased perforin levels with an EC50 value of 7.2 nM.
    In Vivo

    BI-1347 (oral gavage; 10 mg/kg; once daily; 30 d) modulates STAT1 S727 phosphorylation and shows anti-tumor activity in vivo[2].
    BI-1347 (oral gavage; 10 mg/kg) intermittent schedule and BI-8382 continuous treatment combination treatment increases efficacy compared to each monotherapy in the mammary carcinoma EMT6 model[2].

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

    Animal Model: B16-F10-luc2 syngeneic melanoma model[2]
    Dosage: 10 mg/kg
    Administration: Oral gavage; 10 mg/kg; once daily; 30 d
    Result: Reduced phosphorylation of STAT1 S727 for at least 6 h by 60%.
    Showed minimal effect on body weight at 10 mg/kg.
    Showed lower tumor burden both on day 23 and 29, compared to the control group.
    Molecular Weight

    356.42

    Formula

    C22H20N4O
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(N(C)C)CN1N=CC(C2=CC=C(C3=CN=CC4=C3C=CC=C4)C=C2)=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (350.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8057 mL 14.0284 mL 28.0568 mL
    5 mM 0.5611 mL 2.8057 mL 5.6114 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    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: ≥ 2.08 mg/mL (5.84 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.84 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    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).
    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
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8057 mL 14.0284 mL 28.0568 mL 70.1420 mL
    5 mM 0.5611 mL 2.8057 mL 5.6114 mL 14.0284 mL
    10 mM 0.2806 mL 1.4028 mL 2.8057 mL 7.0142 mL
    15 mM 0.1870 mL 0.9352 mL 1.8705 mL 4.6761 mL
    20 mM 0.1403 mL 0.7014 mL 1.4028 mL 3.5071 mL
    25 mM 0.1122 mL 0.5611 mL 1.1223 mL 2.8057 mL
    30 mM 0.0935 mL 0.4676 mL 0.9352 mL 2.3381 mL
    40 mM 0.0701 mL 0.3507 mL 0.7014 mL 1.7535 mL
    50 mM 0.0561 mL 0.2806 mL 0.5611 mL 1.4028 mL
    60 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1690 mL
    80 mM 0.0351 mL 0.1754 mL 0.3507 mL 0.8768 mL
    100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7014 mL
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    BI-1347 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-13472163056-91-3BI1347BI 1347CDKCyclin dependent kinaseoral activityselectivityanti-tumoral activitymouse splenic NK cellhuman NK92MI cellInhibitorinhibitorinhibit

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