GF 109203X

Cat. No. 0741

GF 109203X C25H24N4O2 [133052-90-1]

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Alternative Names: Gö 6850, Bisindolylmaleimide I

Chemical Name: 2-[1-(3-Dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl) maleimide

Biological Activity

Very potent and selective inhibitor of protein kinase C, selective for the α and β1 isoforms (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC50 values are 0.6, 4.6, and 33 μM respectively). Potent antagonist at the 5-HT3 receptor (Ki = 29.5 nM). Anti-inflammatory in vivo.

Technical Data

M.Wt:
412.49
Formula:
C25H24N4O2
Solubility:
Soluble to 25 mM in DMSO
Purity:
>98 %
Storage:
Store at RT
CAS No:
133052-90-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Jiang et al (2011) Heat shock protein 90-mediated inactivation of nuclear factor-κB switches autophagy to apoptosis through becn1 transcriptional inhibition in selenite-induced NB4 cells. Mol.Biol.Cell. 22 1167. PMID: 21346199.

Coultrap et al (1999) Competitive antagonism of the mouse 5-hydroxytryptamine3 receptor by bisindolylmaleimide I, a "selective" protein kinase C inhibitor. J.Pharmacol.Exp.Ther. 290 76. PMID: 10381762.

Jacobson et al (1995) Anti-inflammatory properties of Go 6850: a selective inhibitor of protein kinase C. J.Pharmacol.Exp.Ther. 275 995. PMID: 7473193.

Martiny-Baron et al (1993) Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976. J.Biol.Chem. 268 9194. PMID: 8486620.

Toullec et al (1991) The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J.Biol.Chem. 266 15771. PMID: 1874734.

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Citations are publications that use Tocris products. Selected citations for GF 109203X include:

Al-Bayati et al (2016) Effects of thrombin on insulin signalling and glucose uptake in cultured human myotubes. J.Diabetes Complications. 30 1209. PMID: 27396242 .

Yuan et al (2015) Inhibition of protein kinase C by isojacareubin suppresses hepatocellular carcinoma metastasis and induces apoptosis in vitro and in vivo. Sci Rep 5 12889. PMID: 26245668.

Mitrugno et al (2014) A novel and essential role for FcγRIIa in cancer cell-induced platelet activation. Blood 123 249. PMID: 24258815.

Yu et al (2014) Transactivation of epidermal growth factor receptor through platelet-activating factor/receptor in ovarian cancer cells. J Exp Clin Cancer Res 33 85. PMID: 25261977.

Copits and Swanson (2013) Kainate receptor post-translational modifications differentially regulate association with 4.1N to control activity-dependent receptor endocytosis. J Biol Chem 288 8952. PMID: 23400781.

Jahchan et al (2013) A drug repositioning approach identifies tricyclic antidepressants as inhibitors of small cell lung cancer and other neuroendocrine tumors. Cancer Discov 3 1364. PMID: 24078773.

Hudson et al (2012) Phasic contractions of isolated human myometrium are associated with Rho-kinase (ROCK)-dependent phosphorylation of myosin phosphatase-targeting subunit (MYPT1). Mol Hum Reprod 18 265. PMID: 22155728.

Khuituan et al (2012) Fibroblast growth factor-23 abolishes 1,25-dihydroxyvitamin D3-enhanced duodenal calcium transport in male mice. Am J Physiol Endocrinol Metab 302 E903. PMID: 22275752.

Meotti et al (2012) Inflammatory muscle pain is dependent on the activation of kinin B1 and B2 receptors and intracellular kinase pathways. Br J Pharmacol 166 1127. PMID: 22220695.

Barbaric et al (2011) High-content screening for chemical modulators of embryonal carcinoma cell differentiation and survival. J Biomol Screen 16 603. PMID: 21593487.

Chung et al (2007) IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4. J Endocrinol 194 77. PMID: 17592023.

Zapata et al (2007) Regulation of dopamine transporter function and cell surface expression by D3 dopamine receptors. J Biol Chem 282 35842. PMID: 17923483.

Corsini et al (2003) Induction of adipose differentiation related protein and neutral lipid droplet accumulation in keratinocytes by skin irritants. J Invest Dermatol 121 337. PMID: 12880426.

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Keywords: GF 109203X, supplier, Protein, kinase, C, inhibitors, inhibits, PKC, PKM, Kinase, Kinases, alpha, beta, α, β, GF109203X, Go6850, Go, 6850, Tocris Bioscience, Protein Kinase C Inhibitor products

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