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.

Size Price Stock Quantity  
USD 97 In stock
USD 570 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 19 Publications

Purity & Quality Control

Choose Selective PKC Inhibitors

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 NGrJPXRHfW6ldHnvckBie3OjeR?= NGrDOoYzPCCq MWrQdo91\WO2aX;uJIFo[Wmwc4SgRoFkcWyudYOgZY51cHKjY3nzJIxmfGijbDD0c5hqdi2vZXTpZZRm\CCleYTveI95cWOrdImgbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNiYYPz[ZN{\WRiYYOgZ4hidmenIHnuJJZq[WKrbHn0fUBi\nSncjCyOEBpenNiYomgW3NVOSCmeXWgdoVlfWO2aX;uJIF{e2G7LDDJR|UxRTBwMUmwOVUh|ryP MofaNVc1QDV3MES=
CHO cells NU\IfWF2TnWwY4Tpc44h[XO|YYm= M{HOW2lvcGmkaYTpc44hd2ZiQnHjbYxtfXNiYX70bJJi[2m|IHHueIhz[XhicILveIVkfGm4ZTDhcpRq\2WwIHjldJRidWW{IIDy[U1xd3KnIITvJJBwemViY3;ueoVze2mxbjDpckBEVUd{LXX4dJJme3OrbnegR2hQKGOnbHzz NFjCe2oyQTV2MEe2OC=>

... Click to View More Cell Line Experimental Data
Assay
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, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats. [5]

Protocol

Kinase Assay:

[1]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field
selleck catalog

PKC Signaling Pathway Map

Related PKC Products

  • SD-208 New

    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.

  • LDN-214117 New

    LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.

  • Staurosporine

    Staurosporine is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.

  • Sotrastaurin

    Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2.

    Features:Unlike former PKC inhibitors, Sotrastaurin does not enhance apoptosis of murine T-cell blasts in a model of activation-induced cell death.

  • Go 6983

    Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.

  • Enzastaurin (LY317615)

    Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM in cell-free assays, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3.

  • Go6976

    Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.

  • Bisindolylmaleimide IX (Ro 31-8220 Mesylate)

    Bisindolylmaleimide IX (Ro 31-8220 Mesylate) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1.

  • Dequalinium Chloride

    Dequalinium Chloride is a PKC inhibitor with IC50 of 7-18 μM, and also a selective blocker of apamin-sensitive K+ channels with IC50 of 1.1 μM.

Tags: buy Bisindolylmaleimide I (GF109203X) | Bisindolylmaleimide I (GF109203X) supplier | purchase Bisindolylmaleimide I (GF109203X) | Bisindolylmaleimide I (GF109203X) cost | Bisindolylmaleimide I (GF109203X) manufacturer | order Bisindolylmaleimide I (GF109203X) | Bisindolylmaleimide I (GF109203X) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID