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蚂蚁淘在线 / 品牌中心 / Boston Biochem / Boston Biochem/GF 109203X/0741/10

Boston Biochem/GF 109203X/0741/10

价格
￥1880.00
货号：0741/10
浏览量：127
品牌：Boston Biochem
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商品描述
Product Details
Citations (45)
Reviews (1)
Biological Activity Technical DataBackground Product DatasheetsCalculators

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

Background References

  1. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.Toullec et al.J.Biol.Chem., 1991;266:15771
  2. 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
  3. 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
  4. Anti-inflammatory properties of Go 6850: a selective inhibitor of protein kinase C.Jacobson et al.J.Pharmacol.Exp.Ther., 1995;275:995
  5. Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976.Martiny-Baron et al.J.Biol.Chem., 1993;268:9194

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:

45Citations: 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 Pharmacol2019;23:381
  2. Intracellular emetic signaling evoked by the L-type Ca2+ channel agonist FPL64176 in the least shrew (Cryptotis parva).Authors: ZhongEur J Pharmacol2018;834:157
  3. PKCε Inhibits Neuronal Dendritic Spine Development through Dual Phosphorylation of Ephexin5.Authors: Schaffer Et al.Cell Rep2018;25:2470
  4. Selective modulation of tonically active GABAA receptor functional subgroups by G-proteins and protein kinase C.Authors: O"Neill and Sylantyev2018;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 Physiol2017;313:C118
  6. Dynamic regulation of VEGF-inducible genes by an ERK/ERG/p300 transcriptional network.Authors: Fish Et al.Development2017;144:2428
  7. Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine.Authors: Qu Et al.World J Gastrointest Pathophysiol2016;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 J2016;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 Rep2015;5:12889
  11. Phrenic long-term facilitation requires PKCθ activity within phrenic motor neurons.Authors: Devinney Et al.Int J Mol Sci2015;35:8107
  12. Role of SM22 in the differential regulation of phasic vs. tonic smooth muscle.Authors: Rattan and AliBMC Res Notes2015;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 KanBiochim Biophys Acta2015;1853:2662
  14. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.Authors: Lin Et al.J Neurosci2015;16:5555
  15. Dectin-1 Regulates Hepatic Fibrosis and Hepatocarcinogenesis by Suppressing TLR4 Signaling Pathways.Authors: Seifert Et al.Curr Alzheimer Res2015;13:1909
  16. The ATP-Binding Cassette Transporter-2 (ABCA2) Overexpression Modulates Sphingosine Levels and Transcription of the Amyloid Precursor Protein (APP) Gene.Authors: DavisAm J Physiol Gastrointest Liver Physiol2015;12:847
  17. Non-cell-autonomous mechanism of activity-dependent neurotransmitter switching.Authors: Guemez-Gamboa Et al.Neuron2014;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 Ther2014;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 Res2014;33:85
  20. A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.Authors: Mitrugno Et al.Blood2014;123:249
  21. BDNF-endocannabinoid interactions at neocortical inhibitory synapses require phospholipase C signaling.Authors: ZhaoJ Neurophysiol2014;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 Discov2013;3:1364
  23. Kainate receptor post-translational modifications differentially regulate association with 4.1N to control activity-dependent receptor endocytosis.Authors: Copits and SwansonJ Biol Chem2013;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 A2013;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 Neurosci2012;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 Metab2012;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 Reprod2012;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 Pharmacol2012;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 A2011;31:14024
  30. Platelet-activating factor stimulates sodium-hydrogen exchange in ventricular myocytes.Authors: Ajiro Et al.J Neurosci2011;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 Physiol2011;300:C113
  32. High-content screening for chemical modulators of embryonal carcinoma cell differentiation and survival.Authors: Barbaric Et al.J Biomol Screen2011;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 Cortex2011;108:10556
  34. Proteomic analysis uncovers novel actions of the neurosecretory protein VGF in nociceptive processing.Authors: Riedl Et al.Cell Rep2009;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 Pharmacol2009;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 Pharmacol2008;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 Physiol2007;292:H3079
  38. Regulation of DA transporter function and cell surface expression by D3 DA receptors.Authors: Zapata Et al.J Biol Chem2007;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 JohnstonJ Neurosci2007;27:13926
  40. IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.Authors: Chung Et al.J Endocrinol2007;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 A2006;26:4870
  42. Mechanism of the vascular angiotensin II/α2-adrenoceptor interaction.Authors: Jackson Et al.Am J Physiol Cell Physiol2005;314:1109
  43. Expression and functional role of Rho-kinase in rat urinary bladder smooth muscle.Authors: Wibberley Et al.Br J Pharmacol2003;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 Dermatol2003;121:337
  45. Two distinct signaling pathways in hair cycle induction: Stat3-dependent and -independent pathways.Authors: Sano Et al.J Neurosci2000;97:13824

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GF 109203X blocks PKA effects in hippocampal neurons
By Anonymouson 07/21/2019
Application: Species:Rat

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).

Boston Biochem波士顿生物化学已与IQ Proteomics™合作，为分析您的泛素化蛋白提供定制服务。使用哈佛医学院Gygi实验室开发的泛素绝对定量（AQUA）技术，我们可以对样品中存在的不同泛素连接进行定量表征。