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Bisindolylmaleimide I (GF109203X) PKC inhibitor

Name: Bisindolylmaleimide I (GF109203X)
Brand: Selleck Chemicals
SKU: S7208
Availability: InStock
Rating: 5 (64 reviews)

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.

Chemical Structure

Molecular Weight: 412.48

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Quality Control

Batch: Purity: 99.07%

99.07

Related Targets	TGF-beta/Smad ROCK Bcr-Abl
Other PKC Inhibitors	Darovasertib (LXS196) PMA chemical (Phorbol 12-myristate 13-acetate) Enzastaurin Go 6983 Sotrastaurin (AEB071) Go 6976 Bisindolylmaleimide IX (Ro 31-8220) Mesylate Ruboxistaurin (LY333531) Hydrochloride Rottlerin PKC-theta inhibitor

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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
Click to View More Cell Line Experimental Data

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
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.650mg/ml (4.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.270mg/ml (0.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 5.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	412.48	Formula	C₂₅H₂₄N₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	133052-90-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GO 6850			Smiles	CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54

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 (Cell-free assay) 16 nM PKCβ1 (Cell-free assay) 17 nM PKCα (Cell-free assay) 20 nM PKCγ (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. It also produces reversal activity on P-glycoprotein and MRP-mediated multidrug resistance. PKC inhibition by this compound significantly reduces carbachol-stimulated ERK1/2 activation and the subsequent proliferation of SNU-407 colon cancer cells.
Kinase Assay	Assay of protein kinase C
Kinase Assay	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.).
References	[1] https://pubmed.ncbi.nlm.nih.gov/1874734/ [2] https://pubmed.ncbi.nlm.nih.gov/8826855/ [3] https://pubmed.ncbi.nlm.nih.gov/7818510/ [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		11532940

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Handling Instructions

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