GF 109203X

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Cat.No. 0741 - GF 109203X | C25H24N4O2 | CAS No. 133052-90-1
Description: Protein kinase C inhibitor
Alternative Names: Gö 6850, Bisindolylmaleimide I
Chemical Name: 2-[1-(3-Dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl) maleimide
Purity: ≥98% (HPLC)
Datasheet
Citations (44)
Reviews (1)
Literature

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.

Compound Libraries

GF 109203X is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 412.49
Formula C25H24N4O2
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 133052-90-1
PubChem ID 2396
InChI Key QMGUOJYZJKLOLH-UHFFFAOYSA-N
Smiles CN(C)CCCN1C=C(C2=CC=CC=C12)C1=C(C(=O)NC1=O)C1=CNC2=CC=CC=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.31 25

Preparing Stock Solutions

The following data is based on the product molecular weight 412.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.25 mM 9.7 mL 48.49 mL 96.97 mL
1.25 mM 1.94 mL 9.7 mL 19.39 mL
2.5 mM 0.97 mL 4.85 mL 9.7 mL
12.5 mM 0.19 mL 0.97 mL 1.94 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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

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


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Keywords: GF 109203X, GF 109203X supplier, Protein, kinase, C, inhibitors, inhibits, PKC, PKM, Kinase, Kinases, alpha, beta, α, β, GF109203X, Go6850, Go, 6850, Gö, Bisindolylmaleimide, I, Autophagy, 0741, Tocris Bioscience

44 Citations for GF 109203X

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

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

Riedl et al (2009) Proteomic analysis uncovers novel actions of the neurosecretory protein VGF in nociceptive processing. Cell Rep 29 13377 PMID: 19846725

Wibberley et al (2003) Expression and functional role of Rho-kinase in rat urinary bladder smooth muscle. Br J Pharmacol 138 757 PMID: 12642376

Chen and Kan (2015) Down-regulation of superoxide dismutase 1 by PMA is involved in cell fate determination and mediated via protein kinase D2 in myeloid leukemia cells. Biochim Biophys Acta 1853 2662 PMID: 26241492

Gao et al (2012) Transient receptor potential vanilloid type 1-dependent regulation of liver-related neurons in the paraventricular nucleus of the hypothalamus diminished in the type 1 diabetic mouse. J Neurosci 61 1381 PMID: 22492526

Poteser et al (2011) PKC-dependent coupling of calcium permeation through transient receptor potential canonical 3 (TRPC3) to calcineurin signaling in HL-1 myocytes. Cereb Cortex 108 10556 PMID: 21653882

Lau et al (2011) Apical and basolateral pools of proteinase-activated receptor-2 direct distinct signaling events in the intestinal epithelium. Am J Physiol Heart Circ Physiol 300 C113 PMID: 21068362

Ajiro et al (2011) Platelet-activating factor stimulates sodium-hydrogen exchange in ventricular myocytes. J Neurosci 301 H2395 PMID: 21949111

Zsombok et al (2011) Functional plasticity of central TRPV1 receptors in brainstem dorsal vagal complex circuits of streptozotocin-treated hyperglycemic mice. Proc Natl Acad Sci U S A 31 14024 PMID: 21957263

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

Sano et al (2000) Two distinct signaling pathways in hair cycle induction: Stat3-dependent and -independent pathways. J Neurosci 97 13824 PMID: 11087819

Fish et al (2017) Dynamic regulation of VEGF-inducible genes by an ERK/ERG/p300 transcriptional network. Development 144 2428 PMID: 28536097

Davis (2015) The ATP-Binding Cassette Transporter-2 (ABCA2) Overexpression Modulates Sphingosine Levels and Transcription of the Amyloid Precursor Protein (APP) Gene. Am J Physiol Gastrointest Liver Physiol 12 847 PMID: 26510981

Rattan and Ali (2015) Role of SM22 in the differential regulation of phasic vs. tonic smooth muscle. BMC Res Notes 308 G605 PMID: 25617350

Guemez-Gamboa et al (2014) Non-cell-autonomous mechanism of activity-dependent neurotransmitter switching. Neuron 82 1004 PMID: 24908484

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

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

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

Zhao (2014) BDNF-endocannabinoid interactions at neocortical inhibitory synapses require phospholipase C signaling. J Neurophysiol 111 1008 PMID: 24335212

O'Neill and Sylantyev (2018) Selective modulation of tonically active GABAA receptor functional subgroups by G-proteins and protein kinase C. 243 1046 PMID:  30205722

Schaffer et al (2018) PKCε Inhibits Neuronal Dendritic Spine Development through Dual Phosphorylation of Ephexin5. Cell Rep 25 2470 PMID: 30485813

Jantarajit et al (2017) CFTR-mediated anion secretion across intestinal epithelium-like Caco-2 monolayer under PTH stimulation is dependent on intermediate conductance K+ channels. Am J Physiol Cell Physiol 313 C118 PMID: 28490422

Al-Bayati et al (2016) Effects of thrombin on Ins 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

Freitas et al (2009) Y27632, a Rho-activated kinase inhibitor, normalizes dysregulation in alpha1-adrenergic receptor-induced contraction of Lyon hypertensive rat artery smooth muscle. Fundam Clin Pharmacol 23 169 PMID: 19298234

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 DA transporter function and cell surface expression by D3 DA receptors. J Biol Chem 282 35842 PMID: 17923483

Devinney et al (2015) Phrenic long-term facilitation requires PKCθ activity within phrenic motor neurons. Int J Mol Sci 35 8107 PMID: 26019328

Lin et al (2015) Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals. J Neurosci 16 5555 PMID: 25768340

Seifert et al (2015) Dectin-1 Regulates Hepatic Fibrosis and Hepatocarcinogenesis by Suppressing TLR4 Signaling Pathways. Curr Alzheimer Res 13 1909 PMID: 26655905

Oh et al (2013) Synapse-specific and size-dependent mechanisms of spine structural plasticity accompanying synaptic weakening. Proc Natl Acad Sci U S A 110 E305 PMID: 23269840

Kim et al (2008) Differential enhancement of leukaemia cell differentiation without elevation of intracellular calcium by plant-derived sesquiterpene lactone compounds. Br J Pharmacol 155 814 PMID: 18724384

Cobine et al (2007) Role of L-type calcium channels and PKC in active tone development in rabbit coronary artery. Am J Physiol Heart Circ Physiol 292 H3079 PMID: 17277031

Brager and Johnston (2007) Plasticity of intrinsic excitability during long-term depression is mediated through mGluR-dependent changes in I(h) in hippocampal CA1 pyramidal neurons. J Neurosci 27 13926 PMID: 18094230

Wouters et al (2014) Central role for protein kinase C in oxyt. and epidermal growth factor stimulated cyclooxygenase 2 expression in human myometrial cells. J Pharmacol Exp Ther 7 357 PMID: 24916153

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

O'Riordan et al (2006) Regulation of nuclear factor κB in the hippocampus by group I metabotropic glutamate receptors. Proc Natl Acad Sci U S A 26 4870 PMID: 16672661

Zhong (2018) Intracellular emetic signaling evoked by the L-type Ca2+ channel agonist FPL64176 in the least shrew (Cryptotis parva). Eur J Pharmacol 834 157 PMID: 29966616

Qu et al (2016) Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine. World J Gastrointest Pathophysiol 7 150 PMID: 26909238

Abedini et al (2016) WNT5a is required for normal ovarian follicle development and antagonizes g.tropin responsiveness in granulosa cells by suppressing canonical WNT signaling. FASEB J 30 1534 PMID: 26667040

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

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

Jackson et al (2005) Mechanism of the vascular angiotensin II/α2-adrenoceptor interaction. Am J Physiol Cell Physiol 314 1109 PMID: 15901799


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GF 109203X blocks PKA effects in hippocampal neurons.
By Anonymous on 07/21/2019
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: Hippocampus

GF 109203X (GF-109) was used to clarify an impact of PKC on average open time of GABA-A receptor channel. Experiment on outside-out membrane patches (OOP) and nucleated patches (NP) excised from hippocampal granule cells displayed a significant effect of GF-109 in NPs only. This confirms modulation of GABA-A receptor opening by PKA and ensures absence of GF-109 side effects on GABA-A receptors (since no effect was observed in OOPs).

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