Bisindolylmaleimide I (GF109203X)

Catalog No.S7208 Synonyms: GO 6850 , Bisindolylmaleimide I

Bisindolylmaleimide I (GF109203X) Chemical Structure

Molecular Weight(MW): 412.48

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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2 Customer Reviews

  • (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.

    Cell Death Dis, 2017, 8(2):e2574. Bisindolylmaleimide I (GF109203X) purchased from Selleck.

    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)

    Mol Cell Biochem, 2015, 400(1-2):213-22. . Bisindolylmaleimide I (GF109203X) purchased from Selleck.

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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 MXHGeY5kfGmxbjDhd5NigQ>? NEmzPHAzPCCq NHq0UFZRem:2ZXP0bY9vKGGpYXnud5QhSmGlaXzseZMh[W62aILhZ4l{KGyndHjhcEB1d3irbj3t[YRq[XSnZDDjfZRwfG:6aXPpeJkhcW5ibX;1d4UhWkGZMk[0Mlch[2WubIOgZZN{\XO|ZXSgZZMh[2ijbnflJIlvKH[rYXLpcIl1gSCjZoTldkAzPCCqcoOgZpkhX1OWMTDkfYUhemWmdXP0bY9vKGG|c3H5MEBKSzVyPUCuNVkxPTVizszN NY\SV253OTd2OEW1NFQ>
CHO cells NGDSZnFHfW6ldHnvckBie3OjeR?= MoGzTY5pcWKrdHnvckBw\iCEYXPpcIx2eyCjboTodoFkcXNiYX70bJJigCCycn;0[YN1cX[nIHHueIlo\W5iaHXweIFu\XJicILlMZBwemVidH:gdI9z\SClb372[ZJ{cW:wIHnuJGNOTzJvZYjwdoV{e2mwZzDDTG8h[2WubIO= NYPVUZVqOTl3NEC3OlQ>

... Click to View More Cell Line Experimental Data

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

Protocol

Kinase Assay:

[1]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • Animal Models: Wistar rats
  • Formulation: 10% DMSO in saline
  • 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

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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