Catalog Number: 0741
Alternate 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.
Citations:

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

28 Citations: Showing 1 - 10
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  1. Effects of thrombin on insulin signalling and glucose uptake in cultured human myotubes.
    Authors: Al-Bayati Et al.
    J.Diabetes Complications. 2016;30:1209
  2. 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
  3. Phrenic long-term facilitation requires PKCθ activity within phrenic motor neurons.
    Authors: Devinney Et al.
    Int J Mol Sci 2015;35:8107
  4. Role of SM22 in the differential regulation of phasic vs. tonic smooth muscle.
    Authors: Rattan and Ali
    BMC Res Notes 2015;308:G605
  5. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
    Authors: Lin Et al.
    J Neurosci 2015;16:5555
  6. Dectin-1 Regulates Hepatic Fibrosis and Hepatocarcinogenesis by Suppressing TLR4 Signaling Pathways.
    Authors: Seifert Et al.
    Curr Alzheimer Res 2015;13:1909
  7. 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
  8. 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
  9. 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
  10. A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
    Authors: Mitrugno Et al.
    Blood 2014;123:249
  11. 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
  12. 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
  13. 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
  14. 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
  15. 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
  16. 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
  17. 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
  18. Platelet-activating factor stimulates sodium-hydrogen exchange in ventricular myocytes.
    Authors: Ajiro Et al.
    J Neurosci 2011;301:H2395
  19. 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
  20. High-content screening for chemical modulators of embryonal carcinoma cell differentiation and survival.
    Authors: Barbaric Et al.
    J Biomol Screen 2011;16:603
  21. 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
  22. Proteomic analysis uncovers novel actions of the neurosecretory protein VGF in nociceptive processing.
    Authors: Riedl Et al.
    Cell Rep 2009;29:13377
  23. Regulation of dopamine transporter function and cell surface expression by D3 dopamine receptors.
    Authors: Zapata Et al.
    J Biol Chem 2007;282:35842
  24. IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
    Authors: Chung Et al.
    J Endocrinol 2007;194:77
  25. 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
  26. Mechanism of the vascular angiotensin II/α2-adrenoceptor interaction.
    Authors: Jackson Et al.
    Am J Physiol Cell Physiol 2005;314:1109
  27. 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
  28. Two distinct signaling pathways in hair cycle induction: Stat3-dependent and -independent pathways.
    Authors: Sano Et al.
    J Neurosci 2000;97:13824
Expand to show all 28 Citations

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