2. Epigenetics TGF-beta/Smad Stem Cell/Wnt PI3K/Akt/mTOR
  3. PKC GSK-3
  4. Bisindolylmaleimide I

Bisindolylmaleimide I  (Synonyms: GF109203X; Go 6850)

Cat. No.: HY-13867 Purity: 98.15%
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Bisindolylmaleimide I (GF109203X) is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I is also a GSK-3 inhibitor.

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

CAS No. : 133052-90-1

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10 mM * 1 mL in DMSO
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Customer Review

Based on 40 publication(s) in Google Scholar

Other Forms of Bisindolylmaleimide I:

Bisindolylmaleimide I Related Antibodies

Top Publications Citing Use of Products

40 Publications Citing Use of MCE Bisindolylmaleimide I

WB
Flow Cytometry
Cell Proliferation/Viability Assay
ELISA
Cell Imaging/Staining

    Bisindolylmaleimide I purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2025 Jul 1;20(7):2038-2052.  [Abstract]

    Cell viability was measured by cell counting kit-8 in MN9D cells with/without MPP+ 0.5 mM and Bisindolylmaleimide I (BIM) 5 µM treatment for 24 hours.

    Bisindolylmaleimide I purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2025 Jul 1;20(7):2038-2052.  [Abstract]

    C11-BODIPY fluorescence analysis suggested that MPP+ increased intracellular lipid peroxidation in MN9D cells, and that this effect was reversed by Bisindolylmaleimide I (BIM) (5 μM) treatment.

    Bisindolylmaleimide I purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Mar 11;11(11):5279-5295.  [Abstract]

    SH-SY5Y cells were simultaneously treated with C004019 (1 or 10 µM) and wortmainnin (WO, 1 µM) and Bisindolylmaleimide I (GF-109203X) (GFX, 1 µM) for 24 h to induce tau hyperphosphorylation, and then tau was measured by Western blotting.

    Bisindolylmaleimide I purchased from MedChemExpress. Usage Cited in: Mucosal Immunol. 2022 Feb;15(2):314-326.  [Abstract]

    Lung ILC2s were treated with vehicle or UCB (50 μM) and /or Honokiol (5 μM) and /or Bisindolylmaleimide I (BIM1) (5 μM) in the presence of IL-2, IL-7 and IL-33 for 48 h. Flow cytometric analysis of p-ERK1/2 levels was performed.

    Bisindolylmaleimide I purchased from MedChemExpress. Usage Cited in: Mucosal Immunol. 2022 Feb;15(2):314-326.  [Abstract]

    The amounts of IL-5 and IL-13 in the supernatants were measured by ELISA.

    View All PKC Isoform Specific Products:

    View All Isoforms
    PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

    View All GSK-3 Isoform Specific Products:

    View All Isoforms
    GSK-3 GSK-3α GSK-3β

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Bisindolylmaleimide I (GF109203X) is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I is also a GSK-3 inhibitor[1][2][3].

    IC50 & Target[1]

    Bovine brain PKC

    10 nM (IC50)

    PKCβII

    16 nM (IC50)

    PKCβI

    17 nM (IC50)

    PKCα

    20 nM (IC50)

    PKCγ

    20 nM (IC50)

    FDGFR

    65 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    Platelet IC50
    760 nM
    Compound: 15; GF 109203X
    Inhibition of collagen induced human Platelet aggregation pre-incubated for 1 min followed by collagen stimulation and measured after 30 sec by aggregometer assay
    Inhibition of collagen induced human Platelet aggregation pre-incubated for 1 min followed by collagen stimulation and measured after 30 sec by aggregometer assay
    		[PMID: 1874734]
    Platelet IC50
    875 nM
    Compound: 15; GF 109203X
    Inhibition of alpha-thrombin induced human Platelet aggregation pre-incubated for 1 min followed by alpha-thrombin stimulation and measured after 30 sec by aggregometer assay
    Inhibition of alpha-thrombin induced human Platelet aggregation pre-incubated for 1 min followed by alpha-thrombin stimulation and measured after 30 sec by aggregometer assay
    		[PMID: 1874734]
    RAW264.7 IC50
    1.5 μM
    Compound: GF-109203X
    Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay
    Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay
    		[PMID: 17485504]
    In Vitro

    Bisindolylmaleimide I (5 μM) inhibits α-thrombin-induced P47 phosphorylation[1].
    Bisindolylmaleimide I (0-1 μM) inhibits DNA synthesis in quiescent swiss 3T3 cells[1].
    Bisindolylmaleimide I (5 μM) reduces GSK-3 activity to 25.1±4.3% in adipocytes lysates[3].
    Bisindolylmaleimide I (10 μM, 24 h) inhibits exosome and microvesicle (EMV) release from PC3 cells[4].
    Bisindolylmaleimide I (10 μM, 24 h) enhances cytotoxicity of 5-fluorouracil (HY-90006)[4].

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

    Bisindolylmaleimide I Related Antibodies
    In Vivo

    Bisindolylmaleimide I (0.02 mg/kg, i.p.) reduced the inceased NLRP3, P-PKCɑ, and PKCɑ levels in mechanical ventilation (MV) group in mice[5].
    Bisindolylmaleimide I (0-20 mg/kg, i.p.) reduces the mean frequency of Quinpirole-induced vomiting in shrews[6].

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

    Animal Model: Quinpirole-treated shrews[2]
    Dosage: 0-20 mg/kg
    Administration: i.p.
    Result: Reduced the mean frequency of Quinpirole-induced vomiting.
    Blocked Quinpirole-mediated ERK1/2 phosphorylation in shrew brainstems.
    Molecular Weight

    412.48

    Formula

    C25H24N4O2
    CAS No.
    Appearance

    Solid

    Color

    Pink to red

    SMILES

    O=C(C(C1=CN(CCCN(C)C)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O
    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 : 10 mg/mL (24.24 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 2.4244 mL 12.1218 mL 24.2436 mL
    5 mM 0.4849 mL 2.4244 mL 4.8487 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: ≥ 1 mg/mL (2.42 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
    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
    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
    DMSO 1 mM 2.4244 mL 12.1218 mL 24.2436 mL 60.6090 mL
    5 mM 0.4849 mL 2.4244 mL 4.8487 mL 12.1218 mL
    10 mM 0.2424 mL 1.2122 mL 2.4244 mL 6.0609 mL
    15 mM 0.1616 mL 0.8081 mL 1.6162 mL 4.0406 mL
    20 mM 0.1212 mL 0.6061 mL 1.2122 mL 3.0304 mL
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    Bisindolylmaleimide I 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:

    Bisindolylmaleimide I133052-90-1GF109203X Go 6850Go6850Go 6850Go-6850PKCGSK-3Protein kinase CGlycogen synthase kinase-3Glycogen synthase kinase 3Exosome3T3adipocyte5-fluorouracilP47shrewsInhibitorinhibitorinhibit

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