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 49 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 MYfGeY5kfGmxbjDhd5NigQ>? M4LLZVI1KGi{cx?= MX;Qdo91\WO2aX;uJIFo[Wmwc4SgRoFkcWyudYOgZY51cHKjY3nzJIxmfGijbDD0c5hqdi2vZXTpZZRm\CCleYTveI95cWOrdImgbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNiYYPz[ZN{\WRiYYOgZ4hidmenIHnuJJZq[WKrbHn0fUBi\nSncjCyOEBpenNiYomgW3NVOSCmeXWgdoVlfWO2aX;uJIF{e2G7LDDJR|UxRTFwNd88US=> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzR6NUWwOEc,OTd2OEW1NFQ9N2F-
RAW264.7 MW\GeY5kfGmxbjDhd5NigQ>? MlzlVJJwfGWldHnvckBi\2GrboP0JGJi[2mubIXzJIFvfGi{YXPpd{Bxem:2ZXP0bZZmKGGwdHnn[Y4h[W6mIHzleIhidCC2b4jpck1lcXCqdHjldoliKHSxeHnuJINpcW2ncnnjJJBzd3SnaX6gcYVlcWG2ZXSgZ5l1d3SxeHnjbZR6KGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5 MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzR6NUWwOEc,OTd2OEW1NFQ9N2F-
CHO M3nFRmZ2dmO2aX;uJIF{e2G7 MV;Jcohq[mm2aX;uJI9nKEKjY3nscJV{KGGwdHjyZYNqeyCjboTodoF5KHC{b4TlZ5RqfmViYX70bYdmdiCqZYD0ZY1meiCycnWtdI9z\SC2bzDwc5JmKGOxbo\ldpNqd25iaX6gR21IOi2neIDy[ZN{cW6pIFPIU{Bk\Wyucx?= Ml\OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl3NEC3OlQoRjF7NUSwO|Y1RC:jPh?=
insect cells MYHGeY5kfGmxbjDhd5NigQ>? M13rS|EzOCCvaX7z MY\Jcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiR2PUJJRi\yCOTWTLN{BscW6jc3Wg[I9u[WmwIDixN|MhfG9iNEG1JIFucW6xIHHjbYR{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDpcpNm[3RiY3XscJMhcW6ldXLheIVlKG[xcjCxNlAhdWmwczDifUBz[WSrb33leJJq[yCobIXvdoV{[2WwdDDk[ZRm[3Srb36gZoF{\WRiQ3nzRolwKEurblXBV2UhW1SNLWOxJItqfCCkYYPl[EBie3OjeTygTWM2OD1yLkCwNFE{OTkQvF2= NUixVGJURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPzR4Mz:nQmNpTU2ETEyvZV4>
Sf9 MWnGeY5kfGmxbjDhd5NigQ>? NFrBblI{OCCvaX6= MYLJcohq[mm2aX;uJI9nKEeVS{Pi[ZRiKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGPmPUBk\WyuczD1d4lv\yCJU{GgZZMhe3Wkc4TyZZRmKGGwZDDb[4FudWF|Mm3BWHAh[W[2ZYKgN|AhdWmwIHL5JJNkcW6rdHzsZZRqd25iY3;1cpRqdmduIFnDOVA:OC5zOUC1Oe69VQ>? NYPJeHp2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPzR4Mz:nQmNpTU2ETEyvZV4>
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

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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