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: 98.66%
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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.

Bisindolylmaleimide I Chemical Structure

Bisindolylmaleimide I Chemical Structure

CAS No. : 133052-90-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 85 In-stock
Solid
5 mg USD 77 In-stock
10 mg USD 132 In-stock
25 mg USD 264 In-stock
50 mg USD 495 In-stock
100 mg USD 666 In-stock
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Based on 34 publication(s) in Google Scholar

Other Forms of Bisindolylmaleimide I:

Bisindolylmaleimide I Related Antibodies

Top Publications Citing Use of Products

34 Publications Citing Use of MCE Bisindolylmaleimide I

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)

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 : ≥ 32 mg/mL (77.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

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.

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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
25 mM 0.0970 mL 0.4849 mL 0.9697 mL 2.4244 mL
30 mM 0.0808 mL 0.4041 mL 0.8081 mL 2.0203 mL
40 mM 0.0606 mL 0.3030 mL 0.6061 mL 1.5152 mL
50 mM 0.0485 mL 0.2424 mL 0.4849 mL 1.2122 mL
60 mM 0.0404 mL 0.2020 mL 0.4041 mL 1.0101 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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