GF 109203X

  ( 36 citations )    
Product Datasheet
Catalog Number:0741
Alternate Names:Gö 6850, Bisindolylmaleimide I
Chemical Name:2-[1-(3-Dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl) maleimide
Product Details
Citations (36)
Reviews
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.
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Citations:

The citations listed below are publications that use Tocris products. Selected citations for GF 109203X include:

36 Citations: Showing 1 - 10
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  1. Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine.
    Authors: Qu Et al.
    World J Gastrointest Pathophysiol  2016;7:150
  2. WNT5a is required for normal ovarian follicle development and antagonizes gonadotropin responsiveness in granulosa cells by suppressing canonical WNT signaling.
    Authors: Abedini Et al.
    FASEB J  2016;30:1534
  3. Effects of thrombin on insulin signalling and glucose uptake in cultured human myotubes.
    Authors: Al-Bayati Et al.
    J.Diabetes Complications.  2016;30:1209
  4. 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
  5. Phrenic long-term facilitation requires PKCθ activity within phrenic motor neurons.
    Authors: Devinney Et al.
    Int J Mol Sci  2015;35:8107
  6. Role of SM22 in the differential regulation of phasic vs. tonic smooth muscle.
    Authors: Rattan and Ali
    BMC Res Notes  2015;308:G605
  7. 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
  8. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
    Authors: Lin Et al.
    J Neurosci  2015;16:5555
  9. Dectin-1 Regulates Hepatic Fibrosis and Hepatocarcinogenesis by Suppressing TLR4 Signaling Pathways.
    Authors: Seifert Et al.
    Curr Alzheimer Res  2015;13:1909
  10. The ATP-Binding Cassette Transporter-2 (ABCA2) Overexpression Modulates Sphingosine Levels and Transcription of the Amyloid Precursor Protein (APP) Gene.
    Authors: Davis
    Am J Physiol Gastrointest Liver Physiol  2015;12:847
  11. Non-cell-autonomous mechanism of activity-dependent neurotransmitter switching.
    Authors: Guemez-Gamboa Et al.
    Neuron  2014;82:1004
  12. Central role for protein kinase C in oxytocin and epidermal growth factor stimulated cyclooxygenase 2 expression in human myometrial cells.
    Authors: Wouters Et al.
    J Pharmacol Exp Ther  2014;7:357
  13. 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
  14. A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
    Authors: Mitrugno Et al.
    Blood  2014;123:249
  15. 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
  16. 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
  17. 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
  18. 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
  19. 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
  20. 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
  21. 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
  22. 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
  23. Platelet-activating factor stimulates sodium-hydrogen exchange in ventricular myocytes.
    Authors: Ajiro Et al.
    J Neurosci  2011;301:H2395
  24. 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
  25. High-content screening for chemical modulators of embryonal carcinoma cell differentiation and survival.
    Authors: Barbaric Et al.
    J Biomol Screen  2011;16:603
  26. 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
  27. Proteomic analysis uncovers novel actions of the neurosecretory protein VGF in nociceptive processing.
    Authors: Riedl Et al.
    Cell Rep  2009;29:13377
  28. 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
  29. Regulation of dopamine transporter function and cell surface expression by D3 dopamine receptors.
    Authors: Zapata Et al.
    J Biol Chem  2007;282:35842
  30. 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
  31. IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
    Authors: Chung Et al.
    J Endocrinol  2007;194:77
  32. 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
  33. Mechanism of the vascular angiotensin II/α2-adrenoceptor interaction.
    Authors: Jackson Et al.
    Am J Physiol Cell Physiol  2005;314:1109
  34. Expression and functional role of Rho-kinase in rat urinary bladder smooth muscle.
    Authors: Wibberley Et al.
    Br J Pharmacol  2003;138:757
  35. 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
  36. 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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