Bisindolylmaleimide I (GF109203X)

Catalog No.S7208 Batch:S720802

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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)
Water Insoluble
Ethanol Insoluble
* <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.)

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Biological Activity

Description Bisindolylmaleimide I (GF109203X, GO 6850) is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing 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 GF109203X, as an ATP-competitive PKC inhibitor, prevents platelet aggregation induced by stimuli that activate PKC, and has the potential as a tool for studying the involvement of PKC in signal transduction pathways. [1] GF 109203X produces reversal activity on P-glycoprotein and MRP -mediated multidrug resistance. [2] [3] PKC inhibition by GF109203X significantly reduces carbachol-stimulated ERK1/2 activation and the subsequent proliferation of SNU-407 colon cancer cells. [4]
In vivo GF109203X (10 μg/mouse, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats. [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

    Protein kinase C 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. Inhibitors are 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

Customer Product Validation

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

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

Data from [Data independently produced by , , Front Immunol, 2018, 9:268]

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

Selleck's Bisindolylmaleimide I (GF109203X) has been cited by 64 publications

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
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
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
HDAC Inhibition Restores Response to HER2-Targeted Therapy in Breast Cancer via PHLDA1 Induction [ Int J Mol Sci, 2023, 24(7)6228] PubMed: 37047202
Epicardial Adipose Tissue-Derived Leptin Promotes Myocardial Injury in Metabolic Syndrome Rats Through PKC/NADPH Oxidase/ROS Pathway [ J Am Heart Assoc, 2023, 12(15):e029415] PubMed: 37489731

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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