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company name :
Tocris Bioscience
product type :
chemical
product name :
0741/1
catalog :
0741/1
quantity :
1 mg (also 10 mg)
price :
124 USD
more info or order :
citations: 53
Reference
Wijerathne T, Kim J, Kim M, Kim C, Chae M, Lee S, et al. Onion peel extract and its constituent, quercetin inhibits human Slo3 in a pH and calcium dependent manner. Korean J Physiol Pharmacol. 2019;23:381-392 pubmed publisher
Schaffer T, Smith J, Cook E, Phan T, Margolis S. PKCε Inhibits Neuronal Dendritic Spine Development through Dual Phosphorylation of Ephexin5. Cell Rep. 2018;25:2470-2483.e8 pubmed publisher
O Neill N, Sylantyev S. Feature Article: Selective modulation of tonically active GABAA receptor functional subgroups by G-proteins and protein kinase C. Exp Biol Med (Maywood). 2018;243:1046-1055 pubmed publisher
Zhong W, Chebolu S, Darmani N. Intracellular emetic signaling evoked by the L-type Ca2+ channel agonist FPL64176 in the least shrew (Cryptotis parva). Eur J Pharmacol. 2018;834:157-168 pubmed publisher
Fish J, Cantu Gutierrez M, Dang L, Khyzha N, Chen Z, Veitch S, et al. Dynamic regulation of VEGF-inducible genes by an ERK/ERG/p300 transcriptional network. Development. 2017;144:2428-2444 pubmed publisher
Jantarajit W, Lertsuwan K, Teerapornpuntakit J, Krishnamra N, Charoenphandhu N. CFTR-mediated anion secretion across intestinal epithelium-like Caco-2 monolayer under PTH stimulation is dependent on intermediate conductance K+ channels. Am J Physiol Cell Physiol. 2017;313:C118-C129 pubmed publisher
Chang J, Ni Y, Han L, Sinnett Smith J, Jacamo R, Rey O, et al. Protein kinase D1 (PKD1) phosphorylation on Ser203 by type I p21-activated kinase (PAK) regulates PKD1 localization. J Biol Chem. 2017;292:9523-9539 pubmed publisher
Al Bayati A, Lukka D, Brown A, Walker M. Effects of thrombin on insulin signalling and glucose uptake in cultured human myotubes. J Diabetes Complications. 2016;30:1209-16 pubmed publisher
Qu M, Ji W, Zhao T, Fang C, Mao S, Gao Z. Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine. World J Gastrointest Pathophysiol. 2016;7:150-9 pubmed publisher
Abedini A, Zamberlam G, Lapointe E, Tourigny C, Boyer A, Paquet M, et al. WNT5a is required for normal ovarian follicle development and antagonizes gonadotropin responsiveness in granulosa cells by suppressing canonical WNT signaling. FASEB J. 2016;30:1534-47 pubmed publisher
Seifert L, Deutsch M, Alothman S, Alqunaibit D, Werba G, Pansari M, et al. Dectin-1 Regulates Hepatic Fibrosis and Hepatocarcinogenesis by Suppressing TLR4 Signaling Pathways. Cell Rep. 2015;13:1909-1921 pubmed publisher
Davis W. The ATP-Binding Cassette Transporter-2 (ABCA2) Overexpression Modulates Sphingosine Levels and Transcription of the Amyloid Precursor Protein (APP) Gene. Curr Alzheimer Res. 2015;12:847-59 pubmed
Yuan X, Chen H, Li X, Dai M, Zeng H, Shan L, et al. Inhibition of protein kinase C by isojacareubin suppresses hepatocellular carcinoma metastasis and induces apoptosis in vitro and in vivo. Sci Rep. 2015;5:12889 pubmed publisher
Chen Y, Kan W. Down-regulation of superoxide dismutase 1 by PMA is involved in cell fate determination and mediated via protein kinase D2 in myeloid leukemia cells. Biochim Biophys Acta. 2015;1853:2662-75 pubmed publisher
Devinney M, Fields D, Huxtable A, Peterson T, Dale E, Mitchell G. Phrenic long-term facilitation requires PKCθ activity within phrenic motor neurons. J Neurosci. 2015;35:8107-17 pubmed publisher
Lin T, Lu C, Wu C, Huang S, Wang S. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals. Int J Mol Sci. 2015;16:5555-71 pubmed publisher
Rattan S, Ali M. Role of SM22 in the differential regulation of phasic vs. tonic smooth muscle. Am J Physiol Gastrointest Liver Physiol. 2015;308:G605-12 pubmed publisher
Yan X, Jiang E, Weng H. Activation of toll like receptor 4 attenuates GABA synthesis and postsynaptic GABA receptor activities in the spinal dorsal horn via releasing interleukin-1 beta. J Neuroinflammation. 2015;12:222 pubmed publisher
Carrim N, Walsh T, Consonni A, Torti M, Berndt M, Metharom P. Role of focal adhesion tyrosine kinases in GPVI-dependent platelet activation and reactive oxygen species formation. PLoS ONE. 2014;9:e113679 pubmed publisher
Yu Y, Zhang M, Zhang X, Cai Q, Zhu Z, Jiang W, et al. Transactivation of epidermal growth factor receptor through platelet-activating factor/receptor in ovarian cancer cells. J Exp Clin Cancer Res. 2014;33:85 pubmed publisher
Wouters E, Hudson C, McArdle C, Bernal A. Central role for protein kinase C in oxytocin and epidermal growth factor stimulated cyclooxygenase 2 expression in human myometrial cells. BMC Res Notes. 2014;7:357 pubmed publisher
Guemez Gamboa A, Xu L, Meng D, Spitzer N. Non-cell-autonomous mechanism of activity-dependent neurotransmitter switching. Neuron. 2014;82:1004-16 pubmed publisher
Zhao L, Levine E. BDNF-endocannabinoid interactions at neocortical inhibitory synapses require phospholipase C signaling. J Neurophysiol. 2014;111:1008-15 pubmed publisher
Mitrugno A, Williams D, Kerrigan S, Moran N. A novel and essential role for Fc?RIIa in cancer cell-induced platelet activation. Blood. 2014;123:249-60 pubmed publisher
Li X, Nooh M, Bahouth S. Role of AKAP79/150 protein in ?1-adrenergic receptor trafficking and signaling in mammalian cells. J Biol Chem. 2013;288:33797-812 pubmed publisher
Jahchan N, Dudley J, Mazur P, Flores N, Yang D, Palmerton A, et al. A drug repositioning approach identifies tricyclic antidepressants as inhibitors of small cell lung cancer and other neuroendocrine tumors. Cancer Discov. 2013;3:1364-77 pubmed publisher
Corbett G, Roy A, Pahan K. 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. J Biol Chem. 2013;288:8299-312 pubmed publisher
Copits B, Swanson G. Kainate receptor post-translational modifications differentially regulate association with 4.1N to control activity-dependent receptor endocytosis. J Biol Chem. 2013;288:8952-65 pubmed publisher
Oh W, Hill T, Zito K. Synapse-specific and size-dependent mechanisms of spine structural plasticity accompanying synaptic weakening. Proc Natl Acad Sci U S A. 2013;110:E305-12 pubmed publisher
Lee G, Subramanian N, Kim A, Aksentijevich I, Goldbach Mansky R, Sacks D, et al. The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature. 2012;492:123-7 pubmed publisher
Gao H, Miyata K, Bhaskaran M, Derbenev A, Zsombok A. 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. Diabetes. 2012;61:1381-90 pubmed publisher
Fox J, Sakamuru S, Huang R, Teneva N, Simmons S, Xia M, et al. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death. Proc Natl Acad Sci U S A. 2012;109:5423-8 pubmed publisher
Khuituan P, Teerapornpuntakit J, Wongdee K, Suntornsaratoon P, Konthapakdee N, Sangsaksri J, et al. Fibroblast growth factor-23 abolishes 1,25-dihydroxyvitamin D?-enhanced duodenal calcium transport in male mice. Am J Physiol Endocrinol Metab. 2012;302:E903-13 pubmed publisher
Fung C, Jones S, Ntrakwah A, Naseem K, Farndale R, Mahaut Smith M. 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. Blood. 2012;119:3613-21 pubmed publisher
Meotti F, Campos R, da Silva K, Paszcuk A, Costa R, Calixto J. Inflammatory muscle pain is dependent on the activation of kinin B? and B? receptors and intracellular kinase pathways. Br J Pharmacol. 2012;166:1127-39 pubmed publisher
Hudson C, Heesom K, Lopez Bernal A. Phasic contractions of isolated human myometrium are associated with Rho-kinase (ROCK)-dependent phosphorylation of myosin phosphatase-targeting subunit (MYPT1). Mol Hum Reprod. 2012;18:265-79 pubmed publisher
Zsombok A, Bhaskaran M, Gao H, Derbenev A, Smith B. Functional plasticity of central TRPV1 receptors in brainstem dorsal vagal complex circuits of streptozotocin-treated hyperglycemic mice. J Neurosci. 2011;31:14024-31 pubmed publisher
Ajiro Y, Saegusa N, Giles W, Stafforini D, Spitzer K. Platelet-activating factor stimulates sodium-hydrogen exchange in ventricular myocytes. Am J Physiol Heart Circ Physiol. 2011;301:H2395-401 pubmed publisher
Poteser M, Schleifer H, Lichtenegger M, Schernthaner M, Stockner T, Kappe C, et al. PKC-dependent coupling of calcium permeation through transient receptor potential canonical 3 (TRPC3) to calcineurin signaling in HL-1 myocytes. Proc Natl Acad Sci U S A. 2011;108:10556-61 pubmed publisher
Barbaric I, Jones M, Harley D, Gokhale P, Andrews P. High-content screening for chemical modulators of embryonal carcinoma cell differentiation and survival. J Biomol Screen. 2011;16:603-17 pubmed publisher
Lau C, Lytle C, Straus D, DeFea K. Apical and basolateral pools of proteinase-activated receptor-2 direct distinct signaling events in the intestinal epithelium. Am J Physiol Cell Physiol. 2011;300:C113-23 pubmed publisher
Riedl M, Braun P, Kitto K, ROIKO S, Anderson L, Honda C, et al. Proteomic analysis uncovers novel actions of the neurosecretory protein VGF in nociceptive processing. J Neurosci. 2009;29:13377-88 pubmed publisher
Freitas M, Eto M, Kirkbride J, Schott C, Sassard J, Stoclet J. Y27632, a Rho-activated kinase inhibitor, normalizes dysregulation in alpha1-adrenergic receptor-induced contraction of Lyon hypertensive rat artery smooth muscle. Fundam Clin Pharmacol. 2009;23:169-78 pubmed publisher
Kim S, Danilenko M, Kim T. Differential enhancement of leukaemia cell differentiation without elevation of intracellular calcium by plant-derived sesquiterpene lactone compounds. Br J Pharmacol. 2008;155:814-25 pubmed publisher
Brager D, Johnston D. Plasticity of intrinsic excitability during long-term depression is mediated through mGluR-dependent changes in I(h) in hippocampal CA1 pyramidal neurons. J Neurosci. 2007;27:13926-37 pubmed
Zapata A, Kivell B, Han Y, Javitch J, Bolan E, Kuraguntla D, et al. Regulation of dopamine transporter function and cell surface expression by D3 dopamine receptors. J Biol Chem. 2007;282:35842-54 pubmed
Chung H, Seo S, Moon M, Park S. IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4. J Endocrinol. 2007;194:77-85 pubmed
Cobine C, Callaghan B, Keef K. Role of L-type calcium channels and PKC in active tone development in rabbit coronary artery. Am J Physiol Heart Circ Physiol. 2007;292:H3079-88 pubmed
O Riordan K, Huang I, Pizzi M, Spano P, Boroni F, Egli R, et al. Regulation of nuclear factor kappaB in the hippocampus by group I metabotropic glutamate receptors. J Neurosci. 2006;26:4870-9 pubmed
Jackson E, Gao L, Zhu C. Mechanism of the vascular angiotensin II/alpha2-adrenoceptor interaction. J Pharmacol Exp Ther. 2005;314:1109-16 pubmed
Corsini E, Viviani B, Zancanella O, Lucchi L, Visioli F, Serrero G, et al. Induction of adipose differentiation related protein and neutral lipid droplet accumulation in keratinocytes by skin irritants. J Invest Dermatol. 2003;121:337-44 pubmed
Wibberley A, Chen Z, Hu E, Hieble J, Westfall T. Expression and functional role of Rho-kinase in rat urinary bladder smooth muscle. Br J Pharmacol. 2003;138:757-66 pubmed
Sano S, Kira M, Takagi S, Yoshikawa K, Takeda J, Itami S. Two distinct signaling pathways in hair cycle induction: Stat3-dependent and -independent pathways. Proc Natl Acad Sci U S A. 2000;97:13824-9 pubmed
product information
master code :
741
SKU :
0741/1
product name :
GF 109203X
unit size :
1 mg (also 10 mg)
description :
Protein kinase C inhibitor
target :
Protein Kinase C Inhibitors
category :
Small Molecules
purity :
98%
observed molecular weight :
412.49
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
GF 109203X is a very potent and selective inhibitor of protein kinase C, selective for the and 1 isoforms (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 u M for , 1, , and isoforms respectively). Selective over MLCK, PKG and PKA (IC50 values are 0.6, 4.6, and 33 u M respectively). Potent antagonist at the 5-HT3 receptor (Ki = 29.5 nM). Anti-inflammatory in vivo .
top caption :
Protein kinase C inhibitor
extended description :
Protein kinase C inhibitor
chemical name text :
2-[1-(3-Dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl) maleimide
formula :
C25H24N4O2
formula text :
C25H24N4O2
cas num :
133052-90-1
USD :
124 USD
product details :
Protein kinase C inhibitor
alt names :
G 6850,Bisindolylmaleimide I
storage :
Store at RT
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK