Home TGF-beta/Smad PKC inhibitor Bisindolylmaleimide I (GF109203X)

Bisindolylmaleimide I (GF109203X)

Catalog No.S7208 Synonyms: GO 6850

For research use only.

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.

Bisindolylmaleimide I (GF109203X) Chemical Structure

CAS No. 133052-90-1

Selleck's Bisindolylmaleimide I (GF109203X) has been cited by 48 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.
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
RAW264.7 MVjGeY5kfGmxbjDhd5NigQ>? M3ewU|I1KGi{cx?= M4PKcXBzd3SnY4Tpc44h[WejaX7zeEBD[WOrbHz1d{BidnSqcnHjbZMhdGW2aHHsJJRwgGmwLX3l[IlifGWmIHP5eI91d3irY3n0fUBqdiCvb4Xz[UBTSVd{NkSuO{Bk\WyuczDhd5Nme3OnZDDhd{BkcGGwZ3WgbY4hfmmjYnnsbZR6KGGodHXyJFI1KGi{czDifUBYW1RzIHT5[UBz\WS3Y4Tpc44h[XO|YYmsJGlEPTB;MT61{txO MojSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2OEW1NFQoRjF5NEi1OVA1RC:jPh?=
RAW264.7 NGK4SGlHfW6ldHnvckBie3OjeR?= MnnXVJJwfGWldHnvckBi\2GrboP0JGJi[2mubIXzJIFvfGi{YXPpd{Bxem:2ZXP0bZZmKGGwdHnn[Y4h[W6mIHzleIhidCC2b4jpck1lcXCqdHjldoliKHSxeHnuJINpcW2ncnnjJJBzd3SnaX6gcYVlcWG2ZXSgZ5l1d3SxeHnjbZR6KGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5 MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzR6NUWwOEc,OTd2OEW1NFQ9N2F-
CHO NE\nZndHfW6ldHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKEKjY3nscJV{KGGwdHjyZYNqeyCjboTodoF5KHC{b4TlZ5RqfmViYX70bYdmdiCqZYD0ZY1meiCycnWtdI9z\SC2bzDwc5JmKGOxbo\ldpNqd25iaX6gR21IOi2neIDy[ZN{cW6pIFPIU{Bk\Wyucx?= M{nEVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUSwO|Y1Lz5zOUW0NFc3PDxxYU6=
insect cells NUTlfpRxTnWwY4Tpc44h[XO|YYm= NXHFd2JCOTJyIH3pcpM> M{KyS2lvcGmkaYTpc44hd2ZiTj30[ZJucW6jbDDHV3QhfGGpIFzNWGs{KGurbnHz[UBld22jaX6gLFE{OyC2bzC0NVUh[W2rbn:gZYNq\HNrIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJIlve2WldDDj[YxteyCrbnP1ZoF1\WRiZn;yJFEzOCCvaX7zJIJ6KHKjZHnvcYV1emmlIH\seY9z\XOlZX70JIRmfGWldHnvckBj[XOnZDDDbZNDcW9iS3nuSWFUTSCVVFutV|Ehc2m2IHLhd4VlKGG|c3H5MEBKSzVyPUCuNFAxOTNzON88US=> MkLmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMO|Q3Oy9pPlPoSW1DVDxxYU6=
Sf9 NHLwW|BHfW6ldHnvckBie3OjeR?= NYGwZ2J3OzBibXnu NIHHW2NKdmirYnn0bY9vKG:oIFfTT|Nj\XSjIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJHNnQSClZXzsd{B2e2mwZzDHV|Eh[XNic4Xid5Rz[XSnIHHu[EBc\2GvbXGzNn1CXFBiYX\0[ZIhOzBibXnuJIJ6KHOlaX7peIxt[XSrb36gZ492dnSrbnesJGlEPTB;MD6xPVA2Pc7:TR?= NIW1XJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw4PDZ|Lze+R4hGVUKOPD;hQi=>
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot pMAPK / pCREB / pAKT ; p-HDAC5 / HDAC5 ; p-PKD / PKD 11532940 18332134 16006559
In vivo GF109203X (10 μg/mouse, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats. [5]

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 Research:

[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 Research:

[5]
  • Animal Models: Wistar rats
  • Dosages: 10 μg
  • Administration: i.pl

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 412.48
Formula

C25H24N4O2
CAS No. 133052-90-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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