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Bisindolylmaleimide I

Catalog No. T6513 CAS 133052-90-1

Synonyms: GF109203X, Go 6850

Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor with a Ki of 14 nM.

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Bisindolylmaleimide I Chemical Structure

Bisindolylmaleimide I, CAS 133052-90-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 61.00
10 mg	In stock	$ 101.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 493.00
1 mL * 10 mM (in DMSO)	In stock	$ 66.00

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Purity: 99.08%

Purity: 98.19%

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Description	Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor with a Ki of 14 nM.
Targets&IC50	PKC:14 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]
In vivo	GF109203X (10 μg/mouse, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats. [5]
Kinase Assay	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	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)

Synonyms	GF109203X, Go 6850
Molecular Weight	412.48
Formula	C25H24N4O2
CAS No.	133052-90-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10.3 mg/mL (25 mM)

References and Literature

1. Toullec D, et al. J Biol Chem. 1991, 266(24), 15771-15781. 2. Gekeler V, et al. Br J Cancer. 1996, 74(6), 897-905. 3. Gekeler V, et al. Biochem Biophys Res Commun. 1995, 206(1), 119-126. 4. Park YS, et al. Mol Cell Biochem. 2012, 370(1-2), 191-198. 5. Souza AL, et al. Br J Pharmacol. 2002, 135(1), 239-247. 6. Vetri F, et al. Impairment of neurovascular coupling in Type 1 Diabetes Mellitus in rats is prevented by pancreatic islet transplantation and reversed by a semi-selective PKC inhibitor. Brain Res. 2017 Jan 15;1655:48-54.

Citations

1. Zheng Q, Zou Y, Teng P, et al. Mechanosensitive Channel PIEZO1 Senses Shear Force to Induce KLF2/4 Expression via CaMKII/MEKK3/ERK5 Axis in Endothelial Cells. Cells. 2022, 11(14): 2191

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library TGF-beta/Smad Compound Library Inhibitor Library Highly Selective Inhibitor Library Bioactive Compound Library Angiogenesis related Compound Library Epigenetics Compound Library Anti-Lung Cancer Compound Library

Related Products

Related compounds with same targets

NVP-ACC789 Vorolanib JI-101 AC710 Pazopanib Hydrochloride Tyrosine kinase-IN-1 JNJ-10198409 TAK-632

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Keywords

Bisindolylmaleimide I 133052-90-1 Angiogenesis Chromatin/Epigenetic Cytoskeletal Signaling Tyrosine Kinase/Adaptors PDGFR PKC Go6850 Protein kinase C Go-6850 GF109203X inhibit Go 6850 Inhibitor inhibitor

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