Bisindolylmaleimide I (GF109203X)

For research use only.

Catalog No.S7208 Synonyms: GO 6850

43 publications

Bisindolylmaleimide I (GF109203X) Chemical Structure

CAS No. 133052-90-1

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.

Selleck's Bisindolylmaleimide I (GF109203X) has been cited by 43 publications

Purity & Quality Control

Choose Selective PKC Inhibitors

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.
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.
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
RAW264.7 NIfpd5JHfW6ldHnvckBie3OjeR?= M2[zdlI1KGi{cx?= MkPrVJJwfGWldHnvckBi\2GrboP0JGJi[2mubIXzJIFvfGi{YXPpd{Bt\XSqYXygeI95cW5vbXXkbYF1\WRiY4n0c5RwgGmlaYT5JIlvKG2xdYPlJHJCXzJ4ND63JINmdGy|IHHzd4V{e2WmIHHzJINp[W6pZTDpckB3cWGkaXzpeJkh[W[2ZYKgNlQhcHK|IHL5JHdUXDFiZInlJJJm\HWldHnvckBie3OjeTygTWM2OD1zLkZOwG0> M1TvSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NEi1OVA1Lz5zN{S4OVUxPDxxYU6=
RAW264.7 MULGeY5kfGmxbjDhd5NigQ>? NXfL[2NtWHKxdHXjeIlwdiCjZ3HpcpN1KEKjY3nscJV{KGGwdHjyZYNqeyCycn;0[YN1cX[nIHHueIlo\W5iYX7kJIxmfGijbDD0c5hqdi2maYDoeIhmemmjIITvfIlvKGOqaX3ldolkKHC{b4TlbY4hdWWmaXH0[YQh[3m2b4TvfIlkcXS7IHnuJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6 NVrQVppIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe0PFU2ODRpPkG3OFg2PTB2PD;hQi=>
CHO MXrGeY5kfGmxbjDhd5NigQ>? M1jPW2lvcGmkaYTpc44hd2ZiQnHjbYxtfXNiYX70bJJi[2m|IHHueIhz[XhicILveIVkfGm4ZTDhcpRq\2WwIHjldJRidWW{IIDy[U1xd3KnIITvJJBwemViY3;ueoVze2mxbjDpckBEVUd{LXX4dJJme3OrbnegR2hQKGOnbHzz MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV2MEe2OEc,OTl3NEC3OlQ9N2F-
insect cells M{fDSmZ2dmO2aX;uJIF{e2G7 MlG4NVIxKG2rboO= MXzJcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiR2PUJJRi\yCOTWTLN{BscW6jc3Wg[I9u[WmwIDixN|MhfG9iNEG1JIFucW6xIHHjbYR{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMhcW6ldXLheIVlKG[xcjCxNlAhdWmwczDifUBz[WSrb33leJJq[yCobIXvdoV{[2WwdDDk[ZRm[3Srb36gZoF{\WRiQ3nzRolwKEurblXBV2UhW1SNLWOxJItqfCCkYYPl[EBie3OjeTygTWM2OD1yLkCwNFE{OTkQvF2= NYi3fZkzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPzR4Mz:nQmNpTU2ETEyvZV4>
Sf9 MWDGeY5kfGmxbjDhd5NigQ>? NXTo[24yOzBibXnu M1W2[WlvcGmkaYTpc44hd2ZiR2PLN4JmfGFiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJV{cW6pIFfTNUBieyC|dXLzeJJifGViYX7kJHto[W2vYUOyYWFVWCCjZoTldkA{OCCvaX6gZpkhe2Orbnn0cIxifGmxbjDjc5VvfGmwZzygTWM2OD1yLkG5NFU2|ryP NXvGXplURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPzR4Mz:nQmNpTU2ETEyvZV4>

... Click to View More Cell Line Experimental Data

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, dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats. [5]


Kinase Assay:


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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:


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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:


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  • Animal Models: Wistar rats
  • Dosages: 10 μg
  • Administration:
    (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


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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID