Home / Protein Kinase C Inhibitors / GF 109203X

GF 109203X

Catalog #: 0741
45 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
0741/10
0741/1
GF 109203X | CAS No. 133052-90-1 | Protein Kinase C Inhibitors
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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%

Product Details
Citations (45)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

GF 109203X is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Sodium phenylbutyrate enhances astrocytic neurotrophin synthesis via protein kinase C (PKC)-mediated activation of cAMP-response element-binding protein (CREB): implications for Alzheimer disease therapy.
    Corbett, Grant T, Roy, Avik, Pahan, Kalipada
    J Biol Chem, 2013;288(12):8299-312.
  2. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  3. Activation of toll like receptor 4 attenuates GABA synthesis and postsynaptic GABA receptor activities in the spinal dorsal horn via releasing interleukin-1 beta.
    Yan X, Jiang E, Weng H
    J Neuroinflammation, 2015;12(0):222.
  4. Platelet Ca(2+) responses coupled to glycoprotein VI and Toll-like receptors persist in the presence of endothelial-derived inhibitors: roles for secondary activation of P2X1 receptors and release from intracellular Ca(2+) stores.
    Fung CY, Jones S, Ntrakwah A, Naseem KM, Farndale RW, Mahaut-Smith MP
    Blood, 2012;119(15):3613-21.
  5. Protein kinase D1 (PKD1) phosphorylation on Ser(203) by type I p21-activated kinase (PAK) regulates PKD1 localization
    JK Chang, Y Ni, L Han, J Sinnett-Sm, R Jacamo, O Rey, SH Young, E Rozengurt
    J. Biol. Chem., 2017;0(0):.
  6. A novel and essential role for FcgammaRIIa in cancer cell-induced platelet activation.
    Mitrugno A, Williams D, Kerrigan S, Moran N
    Blood, 2013;123(2):249-60.
  7. Role of focal adhesion tyrosine kinases in GPVI-dependent platelet activation and reactive oxygen species formation.
    Carrim N, Walsh T, Consonni A, Torti M, Berndt M, Metharom P
    PLoS ONE, 2014;9(11):e113679.
  8. The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
    Lee G, Subramanian N, Kim A, Aksentijevich I, Goldbach-Mansky R, Sacks D, Germain R, Kastner D, Chae J
    Nature, 2012;492(7427):123-7.
  9. Role of AKAP79/150 protein in beta1-adrenergic receptor trafficking and signaling in mammalian cells.
    Li X, Nooh M, Bahouth S
    J Biol Chem, 2013;288(47):33797-812.
  10. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.
    Toullec et al.
    J.Biol.Chem., 1991;266:15771
  11. Competitive antagonism of the mouse 5-hydroxytryptamine3 receptor by bisindolylmaleimide I, a "selective" protein kinase C inhibitor.
    Coultrap et al.
    J.Pharmacol.Exp.Ther., 1999;290:76
  12. Anti-inflammatory properties of Go 6850: a selective inhibitor of protein kinase C.
    Jacobson et al.
    J.Pharmacol.Exp.Ther., 1995;275:995
  13. Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976.
    Martiny-Baron et al.
    J.Biol.Chem., 1993;268:9194
  14. 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.
    Mol.Biol.Cell., 2011;22:1167

Product Datasheets

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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

  1. 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
  2. Intracellular emetic signaling evoked by the L-type Ca2+ channel agonist FPL64176 in the least shrew (Cryptotis parva).
    Authors: Zhong
    Eur J Pharmacol  2018;834:157
  3. PKCε Inhibits Neuronal Dendritic Spine Development through Dual Phosphorylation of Ephexin5.
    Authors: Schaffer Et al.
    Cell Rep  2018;25:2470
  4. Selective modulation of tonically active GABAA receptor functional subgroups by G-proteins and protein kinase C.
    Authors: O'Neill and Sylantyev
     2018;243:1046
  5. 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
  6. Dynamic regulation of VEGF-inducible genes by an ERK/ERG/p300 transcriptional network.
    Authors: Fish Et al.
    Development  2017;144:2428
  7. Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine.
    Authors: Qu Et al.
    World J Gastrointest Pathophysiol  2016;7:150
  8. 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
  9. Effects of thrombin on Ins signalling and glucose uptake in cultured human myotubes.
    Authors: Al-Bayati Et al.
    J.Diabetes Complications.  2016;30:1209
  10. 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
  11. Phrenic long-term facilitation requires PKCθ activity within phrenic motor neurons.
    Authors: Devinney Et al.
    Int J Mol Sci  2015;35:8107
  12. Role of SM22 in the differential regulation of phasic vs. tonic smooth muscle.
    Authors: Rattan and Ali
    BMC Res Notes  2015;308:G605
  13. 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
  14. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
    Authors: Lin Et al.
    J Neurosci  2015;16:5555
  15. Dectin-1 Regulates Hepatic Fibrosis and Hepatocarcinogenesis by Suppressing TLR4 Signaling Pathways.
    Authors: Seifert Et al.
    Curr Alzheimer Res  2015;13:1909
  16. 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
  17. Non-cell-autonomous mechanism of activity-dependent neurotransmitter switching.
    Authors: Guemez-Gamboa Et al.
    Neuron  2014;82:1004
  18. 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
  19. 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
  20. A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
    Authors: Mitrugno Et al.
    Blood  2014;123:249
  21. BDNF-endocannabinoid interactions at neocortical inhibitory synapses require phospholipase C signaling.
    Authors: Zhao
    J Neurophysiol  2014;111:1008
  22. 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
  23. 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
  24. 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
  25. 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
  26. 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
  27. 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
  28. 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
  29. 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
  30. Platelet-activating factor stimulates sodium-hydrogen exchange in ventricular myocytes.
    Authors: Ajiro Et al.
    J Neurosci  2011;301:H2395
  31. 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
  32. High-content screening for chemical modulators of embryonal carcinoma cell differentiation and survival.
    Authors: Barbaric Et al.
    J Biomol Screen  2011;16:603
  33. 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
  34. Proteomic analysis uncovers novel actions of the neurosecretory protein VGF in nociceptive processing.
    Authors: Riedl Et al.
    Cell Rep  2009;29:13377
  35. 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
  36. 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
  37. 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
  38. Regulation of DA transporter function and cell surface expression by D3 DA receptors.
    Authors: Zapata Et al.
    J Biol Chem  2007;282:35842
  39. 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
  40. IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
    Authors: Chung Et al.
    J Endocrinol  2007;194:77
  41. 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
  42. Mechanism of the vascular angiotensin II/α2-adrenoceptor interaction.
    Authors: Jackson Et al.
    Am J Physiol Cell Physiol  2005;314:1109
  43. Expression and functional role of Rho-kinase in rat urinary bladder smooth muscle.
    Authors: Wibberley Et al.
    Br J Pharmacol  2003;138:757
  44. 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
  45. 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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