Bisindolylmaleimide I (GF109203X)

For research use only.

Catalog No.S7208 Synonyms: GO 6850 , Bisindolylmaleimide I

28 publications

Bisindolylmaleimide I (GF109203X) Chemical Structure

CAS No. 133052-90-1

Bisindolylmaleimide I (GF109203X) 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.

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Selleck's Bisindolylmaleimide I (GF109203X) has been cited by 28 publications

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Biological Activity

Description Bisindolylmaleimide I (GF109203X) 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.
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.
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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse RAW264.7 cells M1vkNmZ2dmO2aX;uJIF{e2G7 M2PXTlI1KGh? MlfBVJJwfGWldHnvckBi\2GrboP0JGJi[2mubIXzJIFvfGi{YXPpd{Bt\XSqYXygeI95cW5vbXXkbYF1\WRiY4n0c5RwgGmlaYT5JIlvKG2xdYPlJHJCXzJ4ND63JINmdGy|IHHzd4V{e2WmIHHzJINp[W6pZTDpckB3cWGkaXzpeJkh[W[2ZYKgNlQhcHK|IHL5JHdUXDFiZInlJJJm\HWldHnvckBie3OjeTygTWM2OD1yLkG5NFU2KM7:TR?= NHPHbpQyPzR6NUWwOC=>
CHO cells M1;qZWZ2dmO2aX;uJIF{e2G7 MlXRTY5pcWKrdHnvckBw\iCEYXPpcIx2eyCjboTodoFkcXNiYX70bJJigCCycn;0[YN1cX[nIHHueIlo\W5iaHXweIFu\XJicILlMZBwemVidH:gdI9z\SClb372[ZJ{cW:wIHnuJGNOTzJvZYjwdoV{e2mwZzDDTG8h[2WubIO= NF\5U3YyQTV2MEe2OC=>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
pMAPK / pCREB / pAKT ; 

PubMed: 11532940     


The VEGFR- 3-induced p42/p44 MAPK activation is mediated via PKC in HMVECs. Effects of inhibition of PKC by GF109203X (GFX), MEK1 by PD98059, and PI-3 kinase by LY294002 on p42/p44 MAPK Thr202/Tyr204 phosphorylation, CREB Ser133 phosphorylation and Akt Ser473 phosphorylation in HMVECs. The growth factor concentrations used are: VEGF, 1 ng/ml; VEGF-C, 10 ng/ml; and VEGF-C156S, 500 ng/ml.

p-HDAC5 / HDAC5 ; 

PubMed: 18332134     


BAECs were pretreated with vehicle (DMSO as control), PKC inhibitors GF109203X (1–10 μm, C) for 30 min, and then exposed to 20 ng/ml VEGF for 15 min. HDAC5 phosphorylation and expression in cell lysates were determined. Representative immunoblots are shown (n = 3).

p-PKD / PKD ; 

PubMed: 16006559     


BAEC were pretreated with PKC inhibitors GF109203X (A) at the different concentrations for 30 min and then exposed to VEGF (25 ng/ml) for 15 min. PKD activation and expression in cell lysates were determined by Western blot analysis.

11532940 18332134 16006559
In vivo GF109203X (10 μg/mouse, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats. [5]

Protocol

Kinase Assay:

[1]
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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 Research:

[4]
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  • 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.


    (Only for Reference)
Animal Research:

[5]
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  • Animal Models: Wistar rats
  • Dosages: 10 μg
  • Administration: i.pl
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL (198.79 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 412.48
Formula

C25H24N4O2
CAS No. 133052-90-1
Storage powder
in solvent
Synonyms GO 6850 , Bisindolylmaleimide I
Smiles CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID