Chemical Name: 2-[1-(3-Dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl) maleimide
Biological ActivityVery 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.
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.
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.
Toullec et al.
Heat shock protein 90-mediated inactivation of nuclear factor-κB switches autophagy to apoptosis through becn1 transcriptional inhibition in selenite-induced NB4 cells.
Jiang et al.
Competitive antagonism of the mouse 5-hydroxytryptamine3 receptor by bisindolylmaleimide I, a "selective" protein kinase C inhibitor.
Coultrap et al.
Anti-inflammatory properties of Go 6850: a selective inhibitor of protein kinase C.
Jacobson et al.
Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976.
Martiny-Baron et al.
Citations for GF 109203X
The citations listed below are publications that use Tocris products. Selected citations for GF 109203X include:
45 Citations: Showing 1 - 10
Onion peel extract and its constituent, quercetin inhibits human Slo3 in a pH and calcium dependent manner.
Authors: Wijerathne Et al.
Korean J Physiol Pharmacol 2019;23:381
Intracellular emetic signaling evoked by the L-type Ca2+ channel agonist FPL64176 in the least shrew (Cryptotis parva).
Eur J Pharmacol 2018;834:157
PKCε Inhibits Neuronal Dendritic Spine Development through Dual Phosphorylation of Ephexin5.
Authors: Schaffer Et al.
Cell Rep 2018;25:2470
Selective modulation of tonically active GABAA receptor functional subgroups by G-proteins and protein kinase C.
Authors: O'Neill and Sylantyev
CFTR-mediated anion secretion across intestinal epithelium-like Caco-2 monolayer under PTH stimulation is dependent on intermediate conductance K+ channels.
Authors: Jantarajit Et al.
Am J Physiol Cell Physiol 2017;313:C118
Dynamic regulation of VEGF-inducible genes by an ERK/ERG/p300 transcriptional network.
Authors: Fish Et al.
Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine.
Authors: Qu Et al.
World J Gastrointest Pathophysiol 2016;7:150
WNT5a is required for normal ovarian follicle development and antagonizes g.tropin responsiveness in granulosa cells by suppressing canonical WNT signaling.
Authors: Abedini Et al.
FASEB J 2016;30:1534
Effects of thrombin on Ins signalling and glucose uptake in cultured human myotubes.
Authors: Al-Bayati Et al.
J.Diabetes Complications. 2016;30:1209
Inhibition of protein kinase C by isojacareubin suppresses hepatocellular carcinoma metastasis and induces apoptosis in vitro and in vivo.
Authors: Yuan Et al.
Sci Rep 2015;5:12889
Phrenic long-term facilitation requires PKCθ activity within phrenic motor neurons.
Authors: Devinney Et al.
Int J Mol Sci 2015;35:8107
Role of SM22 in the differential regulation of phasic vs. tonic smooth muscle.
Authors: Rattan and Ali
BMC Res Notes 2015;308:G605
Down-regulation of superoxide dismutase 1 by PMA is involved in cell fate determination and mediated via protein kinase D2 in myeloid leukemia cells.
Authors: Chen and Kan
Biochim Biophys Acta 2015;1853:2662
Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
Authors: Lin Et al.
J Neurosci 2015;16:5555
Dectin-1 Regulates Hepatic Fibrosis and Hepatocarcinogenesis by Suppressing TLR4 Signaling Pathways.
Authors: Seifert Et al.
Curr Alzheimer Res 2015;13:1909
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 2015;12:847
Non-cell-autonomous mechanism of activity-dependent neurotransmitter switching.
Authors: Guemez-Gamboa Et al.
Central role for protein kinase C in oxyt. and epidermal growth factor stimulated cyclooxygenase 2 expression in human myometrial cells.
Authors: Wouters Et al.
J Pharmacol Exp Ther 2014;7:357
Transactivation of epidermal growth factor receptor through platelet-activating factor/receptor in ovarian cancer cells.
Authors: Yu Et al.
J Exp Clin Cancer Res 2014;33:85
A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
Authors: Mitrugno Et al.
BDNF-endocannabinoid interactions at neocortical inhibitory synapses require phospholipase C signaling.
J Neurophysiol 2014;111:1008
A drug repositioning approach identifies tricyclic antidepressants as inhibitors of small cell lung cancer and other neuroendocrine tumors.
Authors: Jahchan Et al.
Cancer Discov 2013;3:1364
Kainate receptor post-translational modifications differentially regulate association with 4.1N to control activity-dependent receptor endocytosis.
Authors: Copits and Swanson
J Biol Chem 2013;288:8952
Synapse-specific and size-dependent mechanisms of spine structural plasticity accompanying synaptic weakening.
Authors: Oh Et al.
Proc Natl Acad Sci U S A 2013;110:E305
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.
Authors: Gao Et al.
J Neurosci 2012;61:1381
Fibroblast growth factor-23 abolishes 1,25-dihydroxyvitamin D3-enhanced duodenal calcium transport in male mice.
Authors: Khuituan Et al.
Am J Physiol Endocrinol Metab 2012;302:E903
Phasic contractions of isolated human myometrium are associated with Rho-kinase (ROCK)-dependent phosphorylation of myosin phosphatase-targeting subunit (MYPT1).
Authors: Hudson Et al.
Mol Hum Reprod 2012;18:265
Inflammatory muscle pain is dependent on the activation of kinin B1 and B2 receptors and intracellular kinase pathways.
Authors: Meotti Et al.
Br J Pharmacol 2012;166:1127
Functional plasticity of central TRPV1 receptors in brainstem dorsal vagal complex circuits of streptozotocin-treated hyperglycemic mice.
Authors: Zsombok Et al.
Proc Natl Acad Sci U S A 2011;31:14024
Platelet-activating factor stimulates sodium-hydrogen exchange in ventricular myocytes.
Authors: Ajiro Et al.
J Neurosci 2011;301:H2395
Apical and basolateral pools of proteinase-activated receptor-2 direct distinct signaling events in the intestinal epithelium.
Authors: Lau Et al.
Am J Physiol Heart Circ Physiol 2011;300:C113
High-content screening for chemical modulators of embryonal carcinoma cell differentiation and survival.
Authors: Barbaric Et al.
J Biomol Screen 2011;16:603
PKC-dependent coupling of calcium permeation through transient receptor potential canonical 3 (TRPC3) to calcineurin signaling in HL-1 myocytes.
Authors: Poteser Et al.
Cereb Cortex 2011;108:10556
Proteomic analysis uncovers novel actions of the neurosecretory protein VGF in nociceptive processing.
Authors: Riedl Et al.
Cell Rep 2009;29:13377
Y27632, a Rho-activated kinase inhibitor, normalizes dysregulation in alpha1-adrenergic receptor-induced contraction of Lyon hypertensive rat artery smooth muscle.
Authors: Freitas Et al.
Fundam Clin Pharmacol 2009;23:169
Differential enhancement of leukaemia cell differentiation without elevation of intracellular calcium by plant-derived sesquiterpene lactone compounds.
Authors: Kim Et al.
Br J Pharmacol 2008;155:814
Role of L-type calcium channels and PKC in active tone development in rabbit coronary artery.
Authors: Cobine Et al.
Am J Physiol Heart Circ Physiol 2007;292:H3079
Regulation of DA transporter function and cell surface expression by D3 DA receptors.
Authors: Zapata Et al.
J Biol Chem 2007;282:35842
Plasticity of intrinsic excitability during long-term depression is mediated through mGluR-dependent changes in I(h) in hippocampal CA1 pyramidal neurons.
Authors: Brager and Johnston
J Neurosci 2007;27:13926
IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
Authors: Chung Et al.
J Endocrinol 2007;194:77
Regulation of nuclear factor κB in the hippocampus by group I metabotropic glutamate receptors.
Authors: O'Riordan Et al.
Proc Natl Acad Sci U S A 2006;26:4870
Mechanism of the vascular angiotensin II/α2-adrenoceptor interaction.
Authors: Jackson Et al.
Am J Physiol Cell Physiol 2005;314:1109
Expression and functional role of Rho-kinase in rat urinary bladder smooth muscle.
Authors: Wibberley Et al.
Br J Pharmacol 2003;138:757
Induction of adipose differentiation related protein and neutral lipid droplet accumulation in keratinocytes by skin irritants.
Authors: Corsini Et al.
J Invest Dermatol 2003;121:337
Two distinct signaling pathways in hair cycle induction: Stat3-dependent and -independent pathways.
Authors: Sano Et al.
J Neurosci 2000;97:13824
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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).