Bisindolylmaleimide I (GF109203X)

For research use only.

Catalog No.S7208 Synonyms: GO 6850

35 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.

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Selleck's Bisindolylmaleimide I (GF109203X) has been cited by 35 publications

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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.
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 MWjGeY5kfGmxbjDhd5NigQ>? M2j2R|I1KGi{cx?= NW\IflN1WHKxdHXjeIlwdiCjZ3HpcpN1KEKjY3nscJV{KGGwdHjyZYNqeyCuZYToZYwhfG:6aX6tcYVlcWG2ZXSgZ5l1d3SxeHnjbZR6KGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJIF{e2W|c3XkJIF{KGOqYX7n[UBqdiC4aXHibYxqfHliYX\0[ZIhOjRiaILzJIJ6KFeVVEGg[JlmKHKnZIXjeIlwdiCjc4PhfUwhUUN3ME2xMlXPxE1? NH3qd2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S4OVUxPCd-MUe0PFU2ODR:L3G+
RAW264.7 M3flOmZ2dmO2aX;uJIF{e2G7 MnPSVJJwfGWldHnvckBi\2GrboP0JGJi[2mubIXzJIFvfGi{YXPpd{Bxem:2ZXP0bZZmKGGwdHnn[Y4h[W6mIHzleIhidCC2b4jpck1lcXCqdHjldoliKHSxeHnuJINpcW2ncnnjJJBzd3SnaX6gcYVlcWG2ZXSgZ5l1d3SxeHnjbZR6KGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5 MoPVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2OEW1NFQoRjF5NEi1OVA1RC:jPh?=
CHO M4C5OGZ2dmO2aX;uJIF{e2G7 MVLJcohq[mm2aX;uJI9nKEKjY3nscJV{KGGwdHjyZYNqeyCjboTodoF5KHC{b4TlZ5RqfmViYX70bYdmdiCqZYD0ZY1meiCycnWtdI9z\SC2bzDwc5JmKGOxbo\ldpNqd25iaX6gR21IOi2neIDy[ZN{cW6pIFPIU{Bk\Wyucx?= M2nHe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUSwO|Y1Lz5zOUW0NFc3PDxxYU6=
insect cells NUi5bVBRTnWwY4Tpc44h[XO|YYm= M3K3VVEzOCCvaX7z MVjJcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiR2PUJJRi\yCOTWTLN{BscW6jc3Wg[I9u[WmwIDixN|MhfG9iNEG1JIFucW6xIHHjbYR{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMhcW6ldXLheIVlKG[xcjCxNlAhdWmwczDifUBz[WSrb33leJJq[yCobIXvdoV{[2WwdDDk[ZRm[3Srb36gZoF{\WRiQ3nzRolwKEurblXBV2UhW1SNLWOxJItqfCCkYYPl[EBie3OjeTygTWM2OD1yLkCwNFE{OTkQvF2= M2LV[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFc1PjNxJ{7DbGVOSkx:L3G+
Sf9 MmrrSpVv[3Srb36gZZN{[Xl? M4LWblMxKG2rbh?= MoXSTY5pcWKrdHnvckBw\iCJU1uzZoV1[SBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgeZNqdmdiR2OxJIF{KHO3YoP0doF1\SCjbnSgX4didW2jM{LdRXRRKGGodHXyJFMxKG2rbjDifUB{[2mwaYTscIF1cW:wIHPveY51cW6pLDDJR|UxRTBwMUmwOVXPxE1? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly3OFY{Nyd-Q3jFUWJNRC:jPh?=

... 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