127191-97-3 | KN-62

Packsize	Purity	Availability	Price	Discounted Price
1mg	≥98%	in stock	$63.00	$45.00
5mg	≥98%	in stock	$141.00	$99.00
10mg	≥98%	in stock	$245.00	$171.00
25mg	≥98%	in stock	$519.00	$363.00
100mg	≥98%	in stock	$1,664.00	$1,165.00

Description

• Catalog Number: AA42240
• Chemical Name: KN-62
• CAS Number: 127191-97-3
• Molecular Formula: C38H35N5O6S2
• Molecular Weight: 721.8444
• MDL Number: MFCD00083180
• SMILES: O=C([C@H](Cc1ccc(cc1)OS(=O)(=O)c1cccc2c1ccnc2)NCS(=O)(=O)c1cccc2c1ccnc2)N1CCN(CC1)c1ccccc1

Computed Properties

• Complexity: 1370
• Covalently-Bonded Unit Count: 1
• Defined Atom Stereocenter Count: 1
• Heavy Atom Count: 51
• Hydrogen Bond Acceptor Count: 10
• Rotatable Bond Count: 10
• XLogP3: 5.6

Literature

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  Toxicology in vitro : an international journal published in association with BIBRA 20170401

• Plasticizer DBP Activates NLRP3 Inflammasome through the P2X7 Receptor in HepG2 and L02 Cells.

  Journal of biochemical and molecular toxicology 20160401

• Toluene diisocyanate: Induction of the autotaxin-lysophosphatidic acid axis and its association with airways symptoms.

  Toxicology and applied pharmacology 20150915

• Involvement of CaM-CaMKII-ERK in bisphenol A-induced Sertoli cell apoptosis.

  Toxicology 20141003

• Identification of potent Yes1 kinase inhibitors using a library screening approach.

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• Neuroprotective effect of resveratrol on ischemia/reperfusion injury in rats through TRPC6/CREB pathways.

  Journal of molecular neuroscience : MN 20130701

• A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.

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• Calcium/calmodulin-dependent protein kinase II regulates IL-10 production by human T lymphocytes: a distinct target in the calcium dependent pathway.

  Molecular immunology 20120901

• NOX2-dependent ROS is required for HDAC5 nuclear efflux and contributes to HDAC4 nuclear efflux during intense repetitive activity of fast skeletal muscle fibers.

  American journal of physiology. Cell physiology 20120801

• Pannexin1-mediated ATP release provides signal transmission between Neuro2A cells.

  Neurochemical research 20120601

• Structure-activity relationships and optimization of 3,5-dichloropyridine derivatives as novel P2X(7) receptor antagonists.

  Journal of medicinal chemistry 20120426

• Purinergic P2X7 receptors participate in disturbed intracellular calcium homeostasis in peripheral blood mononuclear cells of patients with chronic kidney disease.

  Kidney & blood pressure research 20120101

• The affinity of histamine for Gq protein-coupled histamine H(1)-receptors is predominantly regulated by their internalization in human astrocytoma cells.

  Journal of pharmacological sciences 20120101

• Exocrine pancreatic carcinogenesis and autotaxin expression.

  PloS one 20120101

• Adipocyte P2X7 receptors expression: a role in modulating inflammatory response in subjects with metabolic syndrome?

  Atherosclerosis 20111201

• CRP1, a protein localized in filopodia of growth cones, is involved in dendritic growth.

  The Journal of neuroscience : the official journal of the Society for Neuroscience 20111116

• Pharmacological properties of the rhesus macaque monkey P2X7 receptor.

  British journal of pharmacology 20110901

• Involvement of histaminergic receptor mechanisms in the stimulation of NT-3 synthesis in astrocytes.

  Neuropharmacology 20110601

• NMDA preconditioning protects against quinolinic acid-induced seizures via PKA, PI3K and MAPK/ERK signaling pathways.

  Behavioural brain research 20110516

• TGF-β-activated kinase 1 mediates mechanical stress-induced IL-6 expression in osteoblasts.

  Biochemical and biophysical research communications 20110506

• Characterization of protoberberine analogs employed as novel human P2X7 receptor antagonists.

  Toxicology and applied pharmacology 20110415

• Requirement for non-regulated, constitutive calcium influx in macrophage survival signaling.

  Biochemical and biophysical research communications 20110408

• LTP in hippocampal neurons is associated with a CaMKII-mediated increase in GluA1 surface expression.

  Journal of neurochemistry 20110201

• Calmodulin and calmodulin-dependent protein kinase II inhibit hormone secretion in human parathyroid adenoma.

  The Journal of endocrinology 20110101

• 4-aminopyridine induces apoptosis of human acute myeloid leukemia cells via increasing [Ca2+]i through P2X7 receptor pathway.

  Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology 20110101

• Targeting P2X₇ receptor inhibits the metastasis of murine P388D1 lymphoid neoplasm cells to lymph nodes.

  Cell biology international 20101201

• Pathways for ATP release by bovine ciliary epithelial cells, the initial step in purinergic regulation of aqueous humor inflow.

  American journal of physiology. Cell physiology 20101201

• TGF-β1 prevents up-regulation of the P2X7 receptor by IFN-γ and LPS in leukemic THP-1 monocytes.

  Biochimica et biophysica acta 20101101

• Mechanism of inhibition of acetylcholine secretion in newly formed mouse synapses involving Ca2+-dependent kinases and voltage-gated K+-channels.

  Bulletin of experimental biology and medicine 20100801

• Osthole or imperatorin-mediated facilitation of glutamate release is associated with a synaptic vesicle mobilization in rat hippocampal glutamatergic nerve endings.

  Synapse (New York, N.Y.) 20100501

• Shockwaves increase T-cell proliferation and IL-2 expression through ATP release, P2X7 receptors, and FAK activation.

  American journal of physiology. Cell physiology 20100301

• Delayed intrinsic activation of an NMDA-independent CaM-kinase II in a critical time window is necessary for late consolidation of an associative memory.

  The Journal of neuroscience : the official journal of the Society for Neuroscience 20100106

• Rebound bursts in GABAergic neurons of the thalamic reticular nucleus in postnatal mice.

  Physiological research 20100101

• Vacuolar ATPase regulates surfactant secretion in rat alveolar type II cells by modulating lamellar body calcium.

  PloS one 20100101

• Defining the antigen receptor-dependent regulatory network that induces arrest of cycling immature B-lymphocytes.

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• Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonists.

  Bioorganic & medicinal chemistry letters 20091101

• Acetylcholine rescues two-cell block through activation of IP3 receptors and Ca2+/calmodulin-dependent kinase II in an ICR mouse strain.

  Pflugers Archiv : European journal of physiology 20091001

• Modulation of K(ATP) currents in rat ventricular myocytes by hypoxia and a redox reaction.

  Acta pharmacologica Sinica 20091001

• Role of calcineurin-mediated dephosphorylation in modulation of an inwardly rectifying K+ channel in human proximal tubule cells.

  The Journal of membrane biology 20091001

• A highly energetic process couples calcium influx through L-type calcium channels to insulin secretion in pancreatic beta-cells.

  American journal of physiology. Endocrinology and metabolism 20090901

• A role for calcium-calmodulin-dependent protein kinase II in the consolidation of visual object recognition memory.

  The European journal of neuroscience 20090901

• P2X7-mediated increased intracellular calcium causes functional derangement in Schwann cells from rats with CMT1A neuropathy.

  The Journal of biological chemistry 20090821

• Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening.

  Bioorganic & medicinal chemistry 20090715

• Up-regulation of ZO-1 expression and barrier function in cultured human corneal epithelial cells by substance P.

  FEBS letters 20090618

• Expression of the dominant-negative tail of myosin Va enhances exocytosis of large dense core vesicles in neurons.

  Cellular and molecular neurobiology 20090601

• Antagonists of the P2X(7) receptor. From lead identification to drug development.

  Journal of medicinal chemistry 20090528

• Activation of ROS/NF-kappaB and Ca2+/CaM kinase II are necessary for VCAM-1 induction in IL-1beta-treated human tracheal smooth muscle cells.

  Toxicology and applied pharmacology 20090515

• The role of P2X7 receptor in ATP-mediated human leukemia cell death: calcium influx-independent.

  Acta biochimica et biophysica Sinica 20090501

• Astrocyte cultures exhibit P2X7 receptor channel opening in the absence of exogenous ligands.

  Glia 20090415

• Synthesis and structure-activity relationships of novel, substituted 5,6-dihydrodibenzo[a,g]quinolizinium P2X7 antagonists.

  Bioorganic & medicinal chemistry letters 20090201

• Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles.

  Journal of medicinal chemistry 20081225

• Destabilization of the postsynaptic density by PSD-95 serine 73 phosphorylation inhibits spine growth and synaptic plasticity.

  Neuron 20081210

• Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects.

  British journal of pharmacology 20081101

• CaMKII-mediated phosphorylation of the myosin motor Myo1c is required for insulin-stimulated GLUT4 translocation in adipocytes.

  Cell metabolism 20081101

• P2X7 receptor-Pannexin1 complex: pharmacology and signaling.

  American journal of physiology. Cell physiology 20080901

• Silencing-induced metaplasticity in hippocampal cultured neurons.

  Journal of neurophysiology 20080801

• Constitutive activity of inwardly rectifying K+ channel at physiological [Ca]i is mediated by Ca2+/CaMK II pathway in opossum kidney proximal tubule cells.

  The journal of physiological sciences : JPS 20080601

• [Effects of chronic hypoxia on the expression of calmodulin and calcicum/calmodulin-dependent protein kinase II and the calcium activity in myocardial cells in young rats].

  Zhongguo dang dai er ke za zhi = Chinese journal of contemporary pediatrics 20080601

• Receptor-mediated tobacco toxicity: acceleration of sequential expression of alpha5 and alpha7 nicotinic receptor subunits in oral keratinocytes exposed to cigarette smoke.

  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20080501

• Induction of nuclear receptors and drug resistance in the brain microvascular endothelial cells treated with antiepileptic drugs.

  Current neurovascular research 20080501

• Depolarization-induced differentiation of PC12 cells is mediated by phospholipase D2 through the transcription factor CREB pathway.

  Journal of neurochemistry 20080301

• A plant Ca2+ pump, ACA2, relieves salt hypersensitivity in yeast. Modulation of cytosolic calcium signature and activation of adaptive Na+ homeostasis.

  The Journal of biological chemistry 20080208

• Role for calcium in the development of ovarial patency in Heliothis virescens.

  Journal of insect physiology 20080201

• Cloning and pharmacological characterization of the guinea pig P2X7 receptor orthologue.

  British journal of pharmacology 20080201

• Negative and positive allosteric modulators of the P2X(7) receptor.

  British journal of pharmacology 20080201

• Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor.

  Bioorganic & medicinal chemistry letters 20080115

• Extracellular ATP mediates necrotic cell swelling in SN4741 dopaminergic neurons through P2X7 receptors.

  The Journal of biological chemistry 20071228

• Functional expression of ionotropic purinergic receptors on mouse taste bud cells.

  The Journal of physiology 20071015

• Behavioral modulation of neuronal calcium/calmodulin-dependent protein kinase II activity: differential effects on nicotine-induced spinal and supraspinal antinociception in mice.

  Biochemical pharmacology 20071015

• Contribution of two ionotropic purinergic receptors to ATP responses in submandibular gland ductal cells.

  Cellular signalling 20071001

• Calcium/calmodulin-dependent kinase activity is required for efficient induction of osteoclast differentiation and bone resorption by receptor activator of nuclear factor kappa B ligand (RANKL).

  Journal of cellular physiology 20070901

• A quantitative method for routine measurement of cell surface P2X7 receptor function in leucocyte subsets by two-colour time-resolved flow cytometry.

  Journal of immunological methods 20070831

• Hepatocyte growth factor-induced enhancement of dendritic branching is blocked by inhibitors of N-methyl-D-aspartate receptors and calcium/calmodulin-dependent kinases.

  Journal of neuroscience research 20070815

• From tyrosine to glycine: synthesis and biological activity of potent antagonists of the purinergic P2X7 receptor.

  Journal of medicinal chemistry 20070726

• KN-62 analogues as potent differentiating agents of HL-60 cells.

  Leukemia research 20070501

• Multiple P2X receptors are involved in the modulation of apoptosis in human mesangial cells: evidence for a role of P2X4.

  American journal of physiology. Renal physiology 20070501

• CaMKII regulates retinoic acid receptor transcriptional activity and the differentiation of myeloid leukemia cells.

  The Journal of clinical investigation 20070501

• Corticotropin-releasing hormone or dexamethasone regulates rat proopiomelanocortin transcription through Tpit/Pitx-responsive element in its promoter.

  The Journal of endocrinology 20070501

• Calcium signalling in the regulation of PGC-1alpha, PDK4 and HKII mRNA expression.

  Biological chemistry 20070501

• Activity-dependent initiation of a prolonged depolarization in aplysia bag cell neurons: role for a cation channel.

  Journal of neurophysiology 20070301

• The select action of hippocampal calcium calmodulin protein kinase II in mediating exercise-enhanced cognitive function.

  Neuroscience 20070209

• Stimulation of adenosine A1 and A2A receptors by AMP in the submucosal plexus of guinea pig small intestine.

  American journal of physiology. Gastrointestinal and liver physiology 20070201

• Microarray-based kinase inhibition assay by gold nanoparticle probes.

  Analytical chemistry 20070115

• Stimulation of fibroblast proliferation by neokyotorphin requires Ca influx and activation of PKA, CaMK II and MAPK/ERK.

  The FEBS journal 20070101

• Life and death in bovine monocytes: the fate of Mycobacterium avium subsp. paratuberculosis.

  Microbial pathogenesis 20070101

• The retinoic acid receptor/CaMKII interaction: pharmacologic inhibition of CaMKII enhances the differentiation of myeloid leukemia cells.

  Blood cells, molecules & diseases 20070101

• Cocaine activates calcium/calmodulin kinase II and causes cardiomyocyte hypertrophy.

  Journal of cardiovascular pharmacology 20060701

• Modulation by LL-37 of the responses of salivary glands to purinergic agonists.

  Molecular pharmacology 20060601

• Microsphere-based protease assays and screening application for lethal factor and factor Xa.

  Cytometry. Part A : the journal of the International Society for Analytical Cytology 20060501

• Activation of P2Y1 receptor triggers two calcium signaling pathways in bone marrow erythroblasts.

  European journal of pharmacology 20060318

• Pore properties and pharmacological features of the P2X receptor channel in airway ciliated cells.

  The Journal of physiology 20060315

• Internalization and desensitization of a green fluorescent protein-tagged P2Y nucleotide receptor are differently controlled by inhibition of calmodulin-dependent protein kinase II.

  Journal of neurochemistry 20060201

• Overexpression of calbindin-D28K in hippocampal progenitor cells increases neuronal differentiation and neurite outgrowth.

  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20060101

• Cocaine inhibition of GABA(A) current: role of dephosphorylation.

  Critical reviews in neurobiology 20060101

• Modulation of intracellular Ca2+ release and capacitative Ca2+ entry by CaMKII inhibitors in bovine vascular endothelial cells.

  American journal of physiology. Cell physiology 20051201

• N-Arylpiperazine modified analogues of the P2X7 receptor KN-62 antagonist are potent inducers of apoptosis of human primary osteoclasts.

  Journal of biomedical science 20051201

• Calcium-acting drugs modulate expression and development of chronic tolerance to nicotine-induced antinociception in mice.

  The Journal of pharmacology and experimental therapeutics 20051101

• Calcium/calmodulin-dependent protein kinase II (CaMKII), through NMDA receptors and L-Voltage-gated channels, modulates the serine phosphorylation of GluR6 during cerebral ischemia and early reperfusion period in rat hippocampus.

  Brain research. Molecular brain research 20051031

• Gonadotropin-releasing hormone induction of extracellular-signal regulated kinase is blocked by inhibition of calmodulin.

  Molecular endocrinology (Baltimore, Md.) 20050901

• Human melanomas express functional P2 X(7) receptors.

  Cell and tissue research 20050901

• Human epidermal and monocyte-derived langerhans cells express functional P2X receptors.

  The Journal of investigative dermatology 20050901

• Netrin-1 induces axon branching in developing cortical neurons by frequency-dependent calcium signaling pathways.

  The Journal of neuroscience : the official journal of the Society for Neuroscience 20050713

• Effects of 17beta-estradiol on chemically induced long-term depression.

  Neuropharmacology 20050701

• Neuroprotective effects of preconditioning ischemia on ischemic brain injury through down-regulating activation of JNK1/2 via N-methyl-D-aspartate receptor-mediated Akt1 activation.

  The Journal of biological chemistry 20050610

• The role of intracellular Ca2+ in the regulation of proteinase-activated receptor-2 mediated nuclear factor kappa B signalling in keratinocytes.

  British journal of pharmacology 20050601

• Activation of CREB by tauroursodeoxycholic acid protects cholangiocytes from apoptosis induced by mTOR inhibition.

  Hepatology (Baltimore, Md.) 20050601

• Decreases in CaMKII activity trigger persistent potentiation of intrinsic excitability in spontaneously firing vestibular nucleus neurons.

  Neuron 20050519

• Nuclear Ca2+ and CaM kinase IV specify hormonal- and Notch-responsiveness.

  Journal of neurochemistry 20050401

• Activity-dependent long-term potentiation of intrinsic excitability in hippocampal CA1 pyramidal neurons.

  The Journal of neuroscience : the official journal of the Society for Neuroscience 20050216

• Somatodendritic autoreceptor regulation of serotonergic neurons: dependence on L-tryptophan and tryptophan hydroxylase-activating kinases.

  The European journal of neuroscience 20050201

• Heterologous desensitization of insulin secretion by GIP (glucose-dependent insulinotropic peptide) in INS-1 cells: the significance of Galphai2 and investigations on the mechanism involved.

  Cell biochemistry and function 20050101

• Extracellular zinc triggers ERK-dependent activation of Na+/H+ exchange in colonocytes mediated by the zinc-sensing receptor.

  The Journal of biological chemistry 20041210

• AMP-activated protein kinase: a new beta-cell glucose sensor?: Regulation by amino acids and calcium ions.

  Diabetes 20041201

• Chlamydophila pneumoniae induces p44/p42 mitogen-activated protein kinase activation in human fibroblasts through Toll-like receptor 4.

  Journal of medical microbiology 20041201

• Synthesis, radiolabeling, and preliminary biological evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X7 receptor.

  Bioorganic & medicinal chemistry letters 20041115

• Extracellular ATP increases cation fluxes in human erythrocytes by activation of the P2X7 receptor.

  The Journal of biological chemistry 20041022

• Mechanisms intrinsic to 5-HT2B receptor-induced potentiation of NMDA receptor responses in frog motoneurones.

  British journal of pharmacology 20041001

• Enhanced P2X7 activity in human fibroblasts from diabetic patients: a possible pathogenetic mechanism for vascular damage in diabetes.

  Arteriosclerosis, thrombosis, and vascular biology 20040701

• Chelerythrine and other benzophenanthridine alkaloids block the human P2X7 receptor.

  British journal of pharmacology 20040701

• Endothelin 1 and 3 enhance neuronal nitric oxide synthase activity through ETB receptors involving multiple signaling pathways in the rat anterior hypothalamus.

  Peptides 20040701

• KN-62, a selective inhibitor of Ca(2+)/calmodulin-dependent protein kinase II, inhibits the lysozyme pre-mRNA splicing in myelomonocytic HD11 cells.

  Biochemical and biophysical research communications 20040625

• Diurnal, circadian and photic regulation of calcium/calmodulin-dependent kinase II and neuronal nitric oxide synthase in the hamster suprachiasmatic nuclei.

  Neurochemistry international 20040601

• Brain ischemia induces serine phosphorylation of neuronal nitric oxide synthase by Ca(2+)/calmodulin-dependent protein kinase II in rat hippocampus.

  Acta pharmacologica Sinica 20040501

• A novel P2X7 receptor activator, the human cathelicidin-derived peptide LL37, induces IL-1 beta processing and release.

  Journal of immunology (Baltimore, Md. : 1950) 20040415

• Signaling pathway of magnolol-stimulated lipolysis in sterol ester-loaded 3T3-L1 preadipocyes.

  Journal of cellular biochemistry 20040401

• Pavlovian fear conditioning regulates Thr286 autophosphorylation of Ca2+/calmodulin-dependent protein kinase II at lateral amygdala synapses.

  The Journal of neuroscience : the official journal of the Society for Neuroscience 20040331

• Ca2+ and AMPK both mediate stimulation of glucose transport by muscle contractions.

  Diabetes 20040201

• Evidence that protein kinase Cdelta is not required for palmitate-induced cytotoxicity in BRIN-BD11 beta-cells.

  Journal of molecular endocrinology 20040201

• Competitive binding of postsynaptic density 95 and Ca2+-calmodulin dependent protein kinase II to N-methyl-D-aspartate receptor subunit 2B in rat brain.

  Acta pharmacologica Sinica 20040201

• A role for calcium/calmodulin kinase in insulin stimulated glucose transport.

  Life sciences 20040102

• NMDA receptor-mediated immediate Ser831 phosphorylation of GluR1 through CaMKIIalpha in rat hippocampus during early global ischemia.

  Neuroscience research 20040101

• Nicotinamide relaxes vascular smooth muscle by inhibiting myosin light chain kinase-dependent signaling pathways: implications for anticancer efficacy.

  Oncology research 20040101

• Agonists and antagonists acting at P2X7 receptor.

  Current topics in medicinal chemistry 20040101

• Dissecting individual current components of co-expressed human P2X1 and P2X7 receptors.

  Current topics in medicinal chemistry 20040101

• Inhibition of lipopolysaccharide/ATP-induced release of interleukin-18 by KN-62 and glyburide.

  European journal of pharmacology 20031215

• Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists.

  Bioorganic & medicinal chemistry letters 20031117

• Dopamine D1 receptors mediate CREB phosphorylation via phosphorylation of the NMDA receptor at Ser897-NR1.

  Journal of neurochemistry 20031101

• Cerebral ischemia immediately increases serine phosphorylation of the synaptic RAS-GTPase activating protein SynGAP by calcium/calmodulin-dependent protein kinase II alpha in hippocampus of rats.

  Neuroscience letters 20031009

• Signalling pathways involved in the sensitisation of mouse nociceptive neurones by nerve growth factor.

  The Journal of physiology 20030901

• Beta-adrenergic stimulation induces cardiac ankyrin repeat protein expression: involvement of protein kinase A and calmodulin-dependent kinase.

  Cardiovascular research 20030901

• Striatal proenkephalin gene induction: coordinated regulation by cyclic AMP and calcium pathways.

  Brain research. Molecular brain research 20030723

• Regulation of ERK phosphorylation by ethanol in fetal cortical neurons.

  Neurochemical research 20030501

• Ca2+/calmodulin-dependent protein kinases II and IV both promote survival but differ in their effects on axon growth in spiral ganglion neurons.

  Journal of neuroscience research 20030415

• Synthesis and biological activity of N-arylpiperazine-modified analogues of KN-62, a potent antagonist of the purinergic P2X7 receptor.

  Journal of medicinal chemistry 20030410

• Insulin-stimulated cyclic guanosine monophosphate inhibits vascular smooth muscle cell migration by inhibiting Ca/calmodulin-dependent protein kinase II.

  Circulation 20030325

• Ameliorative effect of NC-1900, a new AVP4-9 analog, through vasopressin V1A receptor on scopolamine-induced impairments of spatial memory in the eight-arm radial maze.

  Neuropharmacology 20030301

• Calmodulin and calmodulin-dependent kinase II mediate neuronal cell death induced by depolarization.

  Brain research 20030207

• The role of the nuclear receptor CAR as a coordinate regulator of hepatic gene expression in defense against chemical toxicity.

  Archives of biochemistry and biophysics 20030101

• Formation of AP-1 transcription factors during learning in Helix.

  Neuroscience and behavioral physiology 20030101

• A calcium/calmodulin kinase pathway connects brain-derived neurotrophic factor to the cyclic AMP-responsive transcription factor in the rat hippocampus.

  Neuroscience 20030101

• c-IAP1 is overexpressed in HL-60 cells selected for doxorubicin resistance: effects on etoposide-induced apoptosis.

  Anticancer research 20030101

• Synapsin I is phosphorylated at Ser603 by p21-activated kinases (PAKs) in vitro and in PC12 cells stimulated with bradykinin.

  The Journal of biological chemistry 20021122

• Proteasome-driven turnover of tryptophan hydroxylase is triggered by phosphorylation in RBL2H3 cells, a serotonin producing mast cell line.

  European journal of biochemistry 20021001

• Postsynaptic kinase signaling underlies inhibitory synaptic plasticity in the lateral superior olive.

  Journal of neurobiology 20021001

• KN-62 enhances Chlamydia pneumoniae-induced p44/p42 mitogen-activated protein kinase activation in murine fibroblasts and attenuates in vitro infection.

  FEMS microbiology letters 20020924

• Purine and pyrimidine (P2) receptors as drug targets.

  Journal of medicinal chemistry 20020912

• Mechanisms of mitogenic and anti-apoptotic signaling by glucose-dependent insulinotropic polypeptide in beta(INS-1)-cells.

  The Journal of endocrinology 20020801

• Ca(2+)/calmodulin-dependent protein kinase (CaM-kinase) inhibitor KN-62 suppresses the activity of mitogen-activated protein kinase (MAPK), c-myc activation and human keratinocyte proliferation.

  Archives of dermatological research 20020701

• CaMKII regulates amphetamine-induced ERK1/2 phosphorylation in striatal neurons.

  Neuroreport 20020612

• CaMKII is activated and translocated to the secretory apical membrane during cholinergically conveyed gastric acid secretion.

  Cellular signalling 20020201

• Pharmacological characterization of the P2X(7) receptor on human macrophages using the patch-clamp technique.

  Naunyn-Schmiedeberg's archives of pharmacology 20020201

• Protein kinase C increases 11beta-hydroxysteroid dehydrogenase oxidation and inhibits reduction in rat Leydig cells.

  Journal of andrology 20020101

• Synthesis, biological activity and molecular modeling studies of 1,2,3,4-tetrahydroisoquinoline derivatives as conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor containing a tyrosine moiety.

  Arzneimittel-Forschung 20020101

• Effects of calcium, calmodulin, protein kinase C and protein tyrosine kinases on volume-activated taurine efflux in human erythroleukemia cells.

  Journal of cellular physiology 20011201

• Calmodulin and a cyclic nucleotide-dependent protein kinase facilitate the prolactin-induced increase in tyrosine hydroxylase activity in tuberoinfundibular dopaminergic neurons.

  Endocrine 20011101

• Ameliorative effect of vasopressin-(4-9) through vasopressin V(1A) receptor on scopolamine-induced impairments of rat spatial memory in the eight-arm radial maze.

  European journal of pharmacology 20010907

• Functional characterization of P2Y and P2X receptors in human eosinophils.

  Journal of cellular physiology 20010901

• P2Y(11) receptor expression by human lymphocytes: evidence for two cAMP-linked purinoceptors.

  European journal of pharmacology 20010831

• Complex intracellular messenger pathways regulate one type of neuronal alpha-bungarotoxin-resistant nicotinic acetylcholine receptors expressed in insect neurosecretory cells (dorsal unpaired median neurons).

  Molecular pharmacology 20010701

• Glutamate induces focal adhesion kinase tyrosine phosphorylation and actin rearrangement in heterologous mGluR1-expressing CHO cells via calcium/calmodulin signaling.

  Journal of neurochemistry 20010701

• Histamine production by cultured microglial cells of the mouse.

  Neuroscience letters 20010615

• Stimulation of astrocyte-enriched culture with C2 ceramide increases proenkephalin mRNA: involvement of cAMP-response element binding protein and mitogen activated protein kinases.

  Brain research 20010608

• CAMKII inhibition in the parabrachial nuclei elicits conditioned taste aversion in rats.

  Neurobiology of learning and memory 20010501

• Induction of differentiation of human myeloid leukemia cells by immunosuppressant macrolides (rapamycin and FK506) and calcium/calmodulin-dependent kinase inhibitors.

  Experimental hematology 20010501

• Complexities of measuring antagonist potency at P2X(7) receptor orthologs.

  The Journal of pharmacology and experimental therapeutics 20010301

• Modulation of the neuronal dopamine transporter activity by the metabotropic glutamate receptor mGluR5 in rat striatal synaptosomes through phosphorylation mediated processes.

  Journal of neurochemistry 20010301

• The stimulation of MAP kinase by 1,25(OH)(2)-vitamin D(3) in skeletal muscle cells is mediated by protein kinase C and calcium.

  Molecular and cellular endocrinology 20010227

• Inhibition of PP-2A upregulates CaMKII in rat forebrain and induces hyperphosphorylation of tau at Ser 262/356.

  FEBS letters 20010209

• The CEACAM1-L Ser503 residue is crucial for inhibition of colon cancer cell tumorigenicity.

  Oncogene 20010111

• Modulation of choline acetyltransferase synthesis by okadaic acid, a phosphatase inhibitor, and KN-62, a CaM kinase inhibitor, in NS-20Y neuroblastoma.

  Neurochemistry international 20010101

• Effects of extracellular calcium and potassium on the sodium pump of rat adrenal glomerulosa cells.

  American journal of physiology. Cell physiology 20010101

• A proposed mechanism for the potentiation of cAMP-mediated acid secretion by carbachol.

  American journal of physiology. Cell physiology 20010101

• Cell cycle phase specificity in the potentiation of etoposide-induced DNA damage and apoptosis by KN-62, an inhibitor of calcium-calmodulin-dependent enzymes.

  Biochemical pharmacology 20010101

• Calmodulin kinases II and IV and calcineurin are involved in leukemia inhibitory factor-induced cardiac hypertrophy in rats.

  Circulation research 20001110

• Estrogen activation of the nuclear orphan receptor CAR (constitutive active receptor) in induction of the mouse Cyp2b10 gene.

  Molecular endocrinology (Baltimore, Md.) 20001101

• Specificity and mechanism of action of some commonly used protein kinase inhibitors.

  The Biochemical journal 20001001

• Signal-dependent activation of the MEF2 transcription factor by dissociation from histone deacetylases.

  Proceedings of the National Academy of Sciences of the United States of America 20000411

• MAP kinase-independent induction of proto-oncogene c-fos mRNA by hemin in human cells.

  Biochemical and biophysical research communications 19990624

• Effects of antagonists at the human recombinant P2X7 receptor.

  British journal of pharmacology 19980701

• Differential effects of omega-conotoxin GVIA, nimodipine, calmidazolium and KN-62 injected intrathecally on the antinociception induced by beta-endorphin, morphine and [D-Ala2,N-MePhe4,Gly-ol5]-enkephalin administered intracerebroventricularly in the mouse.

  The Journal of pharmacology and experimental therapeutics 19970801

• The isoquinoline derivative KN-62 a potent antagonist of the P2Z-receptor of human lymphocytes.

  British journal of pharmacology 19970401

• Inhibition of sandfly fever Sicilian virus (Phlebovirus) replication in vitro by antiviral compounds.

  Research in virology 19970101

• KN-62, 1-[N,O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazi ne, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II.

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