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

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Bisindolylmaleimide I (GF109203X) PKC inhibitor

Cat.No.S7208

Bisindolylmaleimide I (GF109203X, GO 6850) is a potent PKC inhibitor with IC50 values of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively. This compound shows more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.
Bisindolylmaleimide I (GF109203X) PKC inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 412.48

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RAW264.7 Function assay 24 hrs Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay, IC50=1.5μM 17485504
RAW264.7 Function assay Protection against Bacillus anthracis protective antigen and lethal toxin-diphtheria toxin chimeric protein mediated cytotoxicity in mouse RAW264.7 cells assessed as cell viability 17485504
CHO Function assay Inhibition of Bacillus anthracis anthrax protective antigen heptamer pre-pore to pore conversion in CMG2-expressing CHO cells 19540764
insect cells Function assay 120 mins Inhibition of N-terminal GST tag LMTK3 kinase domain (133 to 415 amino acids) (unknown origin) expressed in insect cells incubated for 120 mins by radiometric fluorescent detection based CisBio KinEASE STK-S1 kit based assay, IC50=0.0001318μM ChEMBL
Sf9 Function assay 30 min Inhibition of GSK3beta (unknown origin) expressed in Sf9 cells using GS1 as substrate and [gamma32]ATP after 30 min by scinitllation counting, IC50=0.19055μM ChEMBL
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Chemical Information, Storage & Stability

Molecular Weight 412.48 Formula

C25H24N4O2

 Storage (From the date of receipt)
CAS No. 133052-90-1 -- Storage of Stock Solutions

Synonyms GO 6850 Smiles CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (198.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

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/IC50/Ki
PKCβ2 [1]
(Cell-free assay)
16 nM
PKCβ1 [1]
(Cell-free assay)
17 nM
PKCα [1]
(Cell-free assay)
20 nM
PKCγ [1]
(Cell-free assay)
20 nM
In vitro
Bisindolylmaleimide I (GF109203X) is an ATP-competitive PKC inhibitor that prevents platelet aggregation induced by stimuli activating PKC, and has potential as a tool for studying PKC involvement in signal transduction pathways. [1] It also produces reversal activity on P-glycoprotein and MRP-mediated multidrug resistance. [2] [3] PKC inhibition by this compound significantly reduces carbachol-stimulated ERK1/2 activation and the subsequent proliferation of SNU-407 colon cancer cells. [4]
Kinase Assay
Assay of protein kinase C
Bisindolylmaleimide I (GF109203X) 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.
In vivo
Bisindolylmaleimide I (GF109203X) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats at a dose of 10 μg/mouse (i.pl.). [5]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/22865467/
  • [5] https://pubmed.ncbi.nlm.nih.gov/11786500/

Applications

Methods Biomarkers Images PMID
Western blot pMAPK / pCREB / pAKT p-HDAC5 / HDAC5 p-PKD / PKD S7208-WB1 11532940

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