Bisindolylmaleimide I (GF109203X)

Catalog No.S7208 Batch:S720801

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Technical Data

Formula

C25H24N4O2
Molecular Weight 412.48 CAS No. 133052-90-1
Solubility (25°C)* In vitro DMSO 82 mg/mL (198.79 mM)
Ethanol 1 mg/mL (2.42 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 1.650mg/ml (4.00mM) Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.270mg/ml (0.65mM) Taking the 1 mL working solution as an example, add 50 μL of 5.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Bisindolylmaleimide I (GF109203X, GO 6850) is a potent PKC inhibitor with IC50 values of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively. This compound shows more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.
Targets
PKCβ2 [1]
(Cell-free assay)		 PKCβ1 [1]
(Cell-free assay)		 PKCα [1]
(Cell-free assay)		 PKCγ [1]
(Cell-free assay)
16 nM 17 nM 20 nM 20 nM
In vitro Bisindolylmaleimide I (GF109203X) is an ATP-competitive PKC inhibitor that prevents platelet aggregation induced by stimuli activating PKC, and has potential as a tool for studying PKC involvement in signal transduction pathways. [1] It also produces reversal activity on P-glycoprotein and MRP-mediated multidrug resistance. [2] [3] PKC inhibition by this compound significantly reduces carbachol-stimulated ERK1/2 activation and the subsequent proliferation of SNU-407 colon cancer cells. [4]
In vivo Bisindolylmaleimide I (GF109203X) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats at a dose of 10 μg/mouse (i.pl.). [5]
Features Greater selectivity than PKC inhibitor staurosporine. GF109203X is a chemical probe for studying PKC signal transduction pathways. Potential for use in a variety of cancers.

Protocol (from reference)

Kinase Assay:

[1]
  • Assay of protein kinase C

    Bisindolylmaleimide I (GF109203X) is arrayed by measuring 32PI transferred from [gamma-32PI] ATP to lysine-rich histone type Ill-s. The reaction mixture (80 μL) contained 50 mM Tris-HCI. pH 7.4, 100 μM CaCl2, 10 mM MgCI2, 37.5 μL/mL histone type Ill-s, 10 μM [gamma-32PI] ATP (1250 cpm/pmol), 31 μM bovine brain phosphatidylserine and 0.5 μM 1,2 sn-dioleylglycerol. Fifteen μL of purified PKC (final concentration in assay 0.38 μg/mL) is added to the incubation mixture. After 10 min at 30°C, the reaction is stopped by addition of 30 μL of casein 30 mg/mL and 0.9 ml of 12% trichloroacetic acid. The acid precipitable material is collected by centrifugation, dissolved in 1N NaOH (100μL) and precipitated again with 1 ml of 12% trichloroacetic acid. The pellet is dissolved in 1N NaOH (100μL) and 32P incorporation is measured by scintillation counting in Aquasol.
Cell Assay:

[4]
  • Cell lines

    SNU-407 colon cancer cells

  • Concentrations

    1 μM

  • Incubation Time

    48 hours

  • Method

    Cell proliferation is monitored by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Cells are seeded in 96-well plates and allowed to grow overnight. The cells are serum-starved for 18–24 hours and then treated with 1 mM carbachol for 48 hours in 100 μL serum-free RPMI 1640. Bisindolylmaleimide I (GF109203X) is added 30 min prior to carbachol treatment. Following the treatment, 10 μL of MTT solution (5 mg/ml) is applied to each well, and the plates were incubated for 3 h at 37 °C. After the medium is removed, the formazan crystals formed are solubilized in 100 μL DMSO. The absorbance at 570 nm is measured using a microplate reader and the background absorbance at 690 nm is subtracted. Each assay is performed in triplicate.
Animal Study:

[5]
  • Animal Models

    Wistar rats

  • Dosages

    10 μg

  • Administration

    i.pl

References

  • https://pubmed.ncbi.nlm.nih.gov/1874734/
  • https://pubmed.ncbi.nlm.nih.gov/8826855/
  • https://pubmed.ncbi.nlm.nih.gov/7818510/
  • https://pubmed.ncbi.nlm.nih.gov/22865467/
  • https://pubmed.ncbi.nlm.nih.gov/11786500/

Customer Product Validation

<p>Effect of PKC inhibitor on DHPG-stimulated Cx43 and ERK1/2 phosphorylation response and GJIC inhibition. Cells were treated with the PKC inhibitor GF109203X (different concentrations indicated) for 30 min prior to DHPG (100 lM, 15 min) treatment. a Representative immunoblots with an anti-Cx43 antibody are shown. b Representative immunoblots with a phospho-specific antibody recognizing the dually phosphorylated form of ERK1/2 (Thr202/Tyr204) and an antibody recognizing total ERK1/2 are shown. Quantitative analysis of the Cx43-P2/Cx43-P0?1 ratio and the phospho-ERK1/2 (p-ERK1/2)/total-ERK1/2 (t-ERK1/2) ratio are shown below the representative immunoblots, respectively. C Cells were incubated without (a) or with 100 lM DHPG (b) or with 100 μM DHPG in combination with 10 μM GF109203X (c) and scrape loaded (9100). d Cells were exposed to GF109203X (different concentrations indicated) alone (filled square) or 100 μM DHPG and GF109203X (filled diamond) prior to measurement of GJIC by scrape loading. Data are shown as mean ± SEM for three separate experiments performed in triplicate (*p<0.05 vs. NC, n = 3, +GF109203X for 0.1, 1, 5 or 10 μM)</p>

, , Mol Cell Biochem, 2015, 400(1-2):213-22.

Effect of MAPK and PKC inhibitors on Nrf2 expression in CWA-treated macrophages.

Data from [ , , Free Radic Biol Med, 2018, 129:338-353 ]

RAW264.7 cells were transfected with Flag-GSTP, followed by pretreatment with or without GF109203X for 2 h, and then stimulated with LPS (500 ng/ml) or phorbol-12-myristate-13-acetate (PMA) for 30 min. Western blot analysis was performed by using anti-p-GSTP (S184) antibody.

Data from [ , , Front Immunol, 2018, 9:268 ]

(b) Western blotting showing that PKC inhibitor increased GLT-1 and GLAST expression in MPP+-treated astrocytes. Results are expressed as the mean±S.E. of at least three experiments. One-way ANOVA. **P<0.01, *P<0.05, #P<0.05. *Represents a significant difference between other group and control group; while #represents a significant difference between the indicated group and MPP+-treated astrocytes for 24 h.

Data from [ , , Cell Death Dis, 2017, 8(2):e2574 ]

Selleck's Bisindolylmaleimide I (GF109203X) Has Been Cited by 68 Publications

Dynamic phosphorylation of Fascin-1 orchestrates microglial phagocytosis and neurological recovery after spinal cord injury [ J Neuroinflammation, 2025, 22(1):121] PubMed: 40281563
HEP14-activated PKC-ERK1/2 pathway boosts HEP14-empowered hADSCs for ovarian regeneration and functional restoration [ Commun Biol, 2025, 8(1):1267] PubMed: 40849553
ELK3 destabilization by speckle-type POZ protein suppresses prostate cancer progression and docetaxel resistance [ Cell Death Dis, 2024, 15(4):274] PubMed: 38632244
Transcription of microRNAs is regulated by developmental signaling pathways and transcription factors [ Front Cell Dev Biol, 2024, 12:1356589] PubMed: 38721525
Downregulation of PIK3IP1/TrIP on T cells is controlled by TCR signal strength, PKC, and metalloprotease-mediated cleavage [ J Biol Chem, 2024, 300(12):107930] PubMed: 39454954
Lysine methylation promotes NFAT5 activation and determines temozolomide efficacy in glioblastoma [ Nat Commun, 2023, 14(1):4062] PubMed: 37429858
Epithelial TNF controls cell differentiation and CFTR activity to maintain intestinal mucin homeostasis [ J Clin Invest, 2023, 10.1172/JCI163591] PubMed: 37643009
Lysine methylation promotes NFAT5 activation and determines temozolomide efficacy in glioblastoma [ Nat Commun, 2023, 14(1):4062] PubMed: 37429858
Neurokinin-1 receptor drives PKCɑ-AURKA/N-Myc signaling to facilitate the neuroendocrine progression of prostate cancer [ Cell Death Dis, 2023, 14(6):384] PubMed: 37385990
Neurokinin-1 receptor drives PKCɑ-AURKA/N-Myc signaling to facilitate the neuroendocrine progression of prostate cancer [ Cell Death Dis, 2023, 14(6):384] PubMed: 37385990

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