LY 294002 hydrochloride
Chemical Name: 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one hydrochloride
Biological ActivityPrototypical PI 3-kinase inhibitor (IC50 values are 0.31, 0.73, 1.06 and 6.60 μM for PI 3-Kβ, PI 3-Kα, PI 3-Kδ and PI 3-Kγ respectively). Also inhibits other kinases including, CK2, mTOR, PLK1, PIM1 and PIM3. Inhibits proliferation and induces apoptosis in human colon cancer cells in vitro and in vivo. Suppresses proliferation of mESCs. Inhibits autophagic sequestration in rat hepatocytes.
Negative Control also available.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
The selectivity of protein kinase inhibitors: a further update.
Bain et al.
Phosphoinositide 3-kinase inhibitor LY294002 but not serum withdrawal suppresses proliferation of murine embryonic stem cells.
Lianguzova et al.
Cell Biol.Int., 2007;31:330
The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes.
Blommaart et al.
A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY 294002).
Vlahos et al.
Citations for LY 294002 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for LY 294002 hydrochloride include:
115 Citations: Showing 1 - 10
Extracorporeal shock waves protect cardiomyocytes from DOX-induced cardiomyopathy by upregulating survivin via the integrin-ILK-Akt-Sp1/p53 axis.
Authors: Lee Et al.
Sci Rep 2019;9:12149
The standardized Korean Red Ginseng extract and its ingredient ginsenoside Rg3 inhibit manifestation of breast cancer stem cell-like properties through modulation of self-renewal signaling.
Authors: Oh Et al.
J Ginseng Res 2019;43:421
Dual RXR motifs regulate nerve growth factor-mediated intracellular retention of the delta opioid receptor.
Authors: Shiwarski Et al.
Mol Biol Cell 2019;30:680
Human vascular cell responses to the circulating bone hormone osteocalcin.
Authors: Millar Et al.
J Cell Physiol 2019;234:21039
The Protective Effect of Ins. on Rat Cortical Neurons in Oxidative Stress and Its Dependence on the Modulation of Akt, GSK-3beta, ERK1/2, and AMPK Activities.
Authors: Zakharova Et al.
Int J Mol Sci 2019;20
Characterization of the brain penetrant neuropeptide Y Y2 receptor antagonist SF-11.
Authors: Domin Et al.
ACS Chem Neurosci 2019;10:3454
Intracellular emetic signaling evoked by the L-type Ca2+ channel agonist FPL64176 in the least shrew (Cryptotis parva).
Authors: Zhong Et al.
Eur J Pharmacol 2018;834:157
The homozygous CX3CR1-M280 mutation impairs human monocyte survival.
Authors: Collar Et al.
JCI Insight 2018;3
PI3Kδ activates E2F1 synthesis in response to mRNA translation stress.
Authors: Gnanasundram Et al.
Nat Commun 2017;8:2103
A pluripotent stem cell-based model for post-implantation human amniotic sac development.
Nat Commun 2017;8(1):208
Structural and pharmacological basis for the induction of mitochondrial biogenesis by formo. but not clenbu.
Sci Rep 2017;7(1):10578
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
PI3K class II α regulates δ-opioid receptor export from the trans-Golgi network.
Authors: Shiwarski Et al.
Mol Biol Cell 2017;28:2202
Phosphoinositide-dependent enrichment of actin monomers in dendritic spines regulates synapse development and plasticity.
Authors: Lei Et al.
J Cell Biol 2017;216:2551
Signaling Cascade Involved in Rapid Stimulation of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by dexameth.
Authors: Bossmann Et al.
Int J Mol Sci 2017;18
Isolation and characterization of a new naturally immortalized human breast carcinoma cell line, KAIMRC1.
Authors: Ali Et al.
BMC Cancer 2017;17:803
Negative regulation of ERK1/2 by PI3K is required for the protective effects of Pyropia yezoensis peptide against perfluorooctane sulfonate-induced endoplasmic reticulum stress.
Authors: Oh Et al.
Mol Med Rep 2017;15:2583
Adenosine A3 receptor elicits chemoresistance mediated by multiple resistance-associated protein-1 in human glioblastoma stem-like cells.
Authors: Torres Et al.
miR-382 targeting PTEN-Akt axis promotes liver regeneration.
Authors: Bei Et al.
The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cellslacking functional GABAB receptors
Authors: Olianas Et al.
European Journal of Pharmacology 2016;794:135
Tumor suppression in basal keratinocytes via dual non-cell-autonomous functions of a Na,K-ATPase beta subunit.
Authors: Hatzold Et al.
Cannabinoid receptor agonist WIN55,212-2 and fatty acid amide hydrolase inhibitor URB597 may protect against cognitive impairment in rats of chronic cerebral hypoperfusion via PI3K/AKT signaling
Authors: Shao-Hua Su Et al.
Behavioural Brain Research 2016;313:334
Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
Authors: Mou Et al.
Cell: Stem Cell 2016;19:217
Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes.
Authors: Liddell Et al.
J Neuroinflammation 2016;13:49
Poly(I:C) increases the expression of mPGES-1 and COX-2 in rat primary microglia.
Authors: Oliveira Et al.
Int J Mol Med 2016;13:11
Progesterone receptor membrane component-1 regulates hepcidin biosynthesis.
Authors: Li Et al.
J Clin Invest 2016;126:389
Up-Regulated Expression of LAMP2 and Autophagy Activity during Neuroendocrine Differentiation of Prostate Cancer LNCaP Cells
Authors: Morell Et al.
PLoS One 2016;11:e0162977
Phosphoinositide-3-Kinase Is the Primary Mediator of Phosphoinositide-Dependent Inhibition in Mammalian Olfactory Receptor Neurons.
Authors: Ukhanov Et al.
Front Cell Neurosci 2016;10:97
Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo.
Authors: Najm Et al.
Int J Cancer 2015;522:216
Integrated β-catenin, BMP, PTEN, and Notch signalling patterns the nephron.
Authors: Lindström Et al.
J Biomed Sci 2015;3:e04000
The thymoquinone-induced production of reactive oxygen species promotes dedifferentiation through the ERK pathway and inflammation through the p38 and PI3K pathways in rabbit articular chondrocytes.
Authors: Yu and Kim
Alcohol Clin Exp Res 2015;35:325
Acetate supplementation as a means of inducing glioblastoma stem-like cell growth arrest.
Authors: Long Et al.
J Cell Physiol 2015;230:1929
Dimeric dipeptide mimetics of the nerve growth factor Loop 4 and Loop 1 activate TRKA with different patterns of intracellular signal transduction.
Authors: Gudasheva Et al.
PI3K Phosphorylation Is Linked to Improved Electrical Excitability in an In Vitro Engineered Heart Tissue Disease Model System.
Authors: Kana Et al.
Tissue Eng Part A 2015;21:2379
Neuregulin 1 signalling modulates mGluR1 function in mesencephalic dopaminergic neurons.
Authors: Ledonne Et al.
Mol Psychiatry 2015;20:959
A novel mechanism for cytoprotection against hypoxic injury: δ-opioid receptor-mediated increase in Nrf2 translocation.
Authors: Cao Et al.
SDF-1α stiffens myeloma bone marrow mesenchymal stromal cells through the activation of RhoA-ROCK-Myosin II.
Authors: Choi Et al.
PLoS One 2015;136:E219
An in vitro model of latency and reactivation of varicella zoster virus in human stem cell-derived neurons.
Authors: Markus Et al.
PLoS Pathog 2015;11:e1004885
Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways.
Authors: Rogers and Gahring
J Neuroinflammation 2015;10:e0143319
Glucocorticoids Distinctively Modulate the CFTR Channel with Possible Implications in Lung Development and Transition into Extrauterine Life.
Authors: Laube Et al.
PLoS One 2015;10:e0124833
Palladin mediates stiffness-induced fibroblast activation in the tumor microenvironment.
Authors: McLane and Ligon
Biophys J 2015;109:249
ER-α36-mediated rapid estrogen signaling positively regulates ER-positive breast cancer stem/progenitor cells.
Authors: Deng Et al.
BMC Cancer 2014;9:e88034
Angiogenic growth factors augment K-Cl cotransporter expression in erythroid cells via hypoxia-inducible factor-1α.
Authors: Gonsalves Et al.
Am J Hematol 2014;89:273
Non-cell-autonomous mechanism of activity-dependent neurotransmitter switching.
Authors: Guemez-Gamboa Et al.
Interaction of mTOR and Erk1/2 signaling to regulate oligodendrocyte differentiation.
Authors: Dai Et al.
Rapid elevation of sodium transport through Ins is mediated by AKT in alveolar cells.
Authors: Mattes Et al.
Physiol Rep 2014;2:e00269
Decrease of PKB/Akt Phosphorylation is Partially Mediated by SAPK/JNK Activation in Serum-free L6 Myoblasts Starved with Low Glucose.
Authors: Kim Et al.
J Phys Ther Sci 2014;26:1757
δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
Authors: Liang Et al.
J Exp Bot 2014;171:5417
BDNF-endocannabinoid interactions at neocortical inhibitory synapses require phospholipase C signaling.
J Neurophysiol 2014;111:1008
Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-DA-like G protein-coupled receptor.
Authors: Bayliss and Evans
PLoS One 2013;8:e80833
Acetate supplementation induces growth arrest of NG2/PDGFRα-positive oligodendroglioma-derived tumor-initiating cells.
Authors: Long Et al.
PLoS One 2013;8:e80714
Curcumin suppresses migration and proliferation of Hep3B hepatocarcinoma cells through inhibition of the Wnt signaling pathway.
Authors: Kim Et al.
Mol Med Rep 2013;8:282
ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change.
Authors: Montané and Menand
PI3K-Akt signaling activates mTOR-mediated epileptogenesis in organotypic hippocampal culture model of post-traumatic epilepsy.
Authors: Berdichevsky Et al.
J Neurosci 2013;33:9056
Melatonin acts through MT1/MT2 receptors to activate hypothalamic Akt and suppress hepatic gluconeogenesis in rats.
Authors: Faria Et al.
Am J Physiol Endocrinol Metab 2013;305:E230
Cellular Ins resistance disrupts leptin-mediated control of neuronal signaling and transcription.
Authors: Nazarians-Armavil Et al.
Mol Endocrinol 2013;27:990
Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family.
Authors: Morse Et al.
BMC Pharmacol Toxicol 2013;14:17
Activation of AMPK inhibits cervical cancer cell growth through AKT/FOXO3a/FOXM1 signaling cascade.
Authors: Yung Et al.
J Steroid Biochem Mol Biol 2013;13:327
PI 3-kinase independent role for AKT in F-actin regulation during outer segment phagocytosis by RPE cells.
Authors: Bulloj Et al.
Exp Eye Res 2013;113:9
Melatonin induces transcriptional regulation of Bim by FoxO3a in HepG2 cells.
Authors: Carbajo-Pescador Et al.
Br J Cancer 2013;108:442
Ceramide 1-phosphate stimulates proliferation of C2C12 myoblasts.
Authors: Gangoiti Et al.
Fucoidan from seaweed Fucus vesiculosus inhibits migration and invasion of human lung cancer cell via PI3K-Akt-mTOR pathways.
Authors: Lee Et al.
PLoS One 2012;7:e50624
PPARδ activation protects endothelial function in diabetic mice.
Authors: Tian Et al.
PI3K/Akt signaling pathway in the basolateral amygdala mediates the rapid antidepressant-like effects of trefoil factor 3.
Authors: Shi Et al.
Nucleus accumbens mGluR5-associated signaling regulates binge alcohol drinking under drinking-in-the-dark procedures.
Authors: Cozzoli Et al.
Cancer Res 2012;36:1623
Cervical spinal erythropoietin induces phrenic motor facilitation via extracellular signal-regulated protein kinase and Akt signaling.
Authors: Dale Et al.
J Neurosci 2012;32:5973
Curcumin inhibits HCV replication by induction of heme oxygenase-1 and suppression of AKT.
Authors: Chen Et al.
Int J Mol Med 2012;30:1021
A screen for regulators of survival of motor neuron protein levels.
Authors: Makhortova Et al.
Nat Chem Biol 2011;7:544
Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target.
Authors: Morse Et al.
PLoS One 2011;6:e25643
Astragaloside IV stimulates angiogenesis and increases hypoxia-inducible factor-1α accumulation via phosphatidylinositol 3-kinase/Akt pathway.
Authors: Zhang Et al.
J Pharmacol Exp Ther 2011;338:485
The canonical nuclear factor-κB pathway regulates cell survival in a developmental model of spinal cord motoneurons.
Authors: Mincheva Et al.
J Neurosci 2011;31:6493
JNK suppression is essential for 17β-OE inhibits prostaglandin E2-Induced uPA and MMP-9 expressions and cell migration in human LoVo colon cancer cells.
Authors: Hsu Et al.
J Med Food 2011;18:61
A positive cross-regulation of HER2 and ER-α36 controls ALDH1 positive breast cancer cells.
Authors: Kang Et al.
J Pharmacol Exp Ther 2011;127:262
Neurotoxicity induced by okadaic acid in the human neuroblastoma SH-SY5Y line can be differentially prevented by α7 and β2* nicotinic stimulation.
Authors: Barrio Et al.
Toxicol Sci 2011;123:193
TRPV4-mediated calcium influx into human bronchial epithelia upon exposure to diesel exhaust particles.
Authors: Li Et al.
Environ Health Perspect 2011;119:784
Cortical overexpression of neuronal calcium sensor-1 induces functional plasticity in spinal cord following unilateral pyramidal tract injury in rat.
Authors: Yip Et al.
PLoS Biol 2010;8:e1000399
Extranuclear estrogen receptors mediate the neuroprotective effects of estrogen in the rat hippocampus.
Authors: Yang Et al.
PLoS One 2010;5:e9851
Pharmacological and genetic accumulation of hypoxia-inducible factor-1alpha enhances excitatory synaptic transmission in hippocampal neurons through the production of vascular endothelial growth factor.
Authors: Huang Et al.
J Neurosci 2010;30:6080
Leptin regulates AMPA receptor trafficking via PTEN inhibition.
Authors: Moult Et al.
J Neurosci 2010;30:4088
Mechano-transduction in osteoblastic cells involves strain-regulated estrogen receptor alpha-mediated control of Ins-like growth factor (IGF) I receptor sensitivity to Ambient IGF, leading to phosphatidylinositol 3-kinase/AKT-dependent Wnt/LRP5 receptor-i
Authors: Sunters Et al.
J Biol Chem 2010;285:8743
miR-155 and its star-form partner miR-155* cooperatively regulate type I IF. production by human plasmacytoid dendritic cells.
Authors: Zhou Et al.
Level of G protein-coupled receptor kinase-2 determines myocardial ischemia/reperfusion injury via pro- and anti-apoptotic mechanisms.
Authors: Brinks Et al.
J Cell Sci 2010;107:1140
Optimal experimental design for parameter estimation of a cell signaling model.
Authors: Bandara Et al.
PLoS Comput Biol 2009;5:e1000558
FcεRI-induced activation by low antigen concentrations results in nuclear signals in the absence of degranulation.
Authors: Grodzki Et al.
Circ Res 2009;46:2539
Activation of glycogen synthase kinase-3 β is required for hyperDA and D2 receptor-mediated inhibition of synaptic NMDA receptor function in the rat prefrontal cortex.
Authors: Li Et al.
J Biol Chem 2009;29:15551
Regulation of p53 expression, phosphorylation and subcellular localization by a G-protein-coupled receptor.
Authors: Solyakov Et al.
PLZF is a regulator of homeostatic and cytokine-induced myeloid development.
Authors: Doulatov Et al.
Genes Dev 2009;23:2076
Glycogen synthase kinase-3 and Omi/HtrA2 induce annexin A2 cleavage followed by cell cycle inhibition and apoptosis.
Authors: Wang Et al.
Mol Biol Cell 2009;20:4153
Ethanol augments RANTES/CCL5 expression in rat liver sinusoidal endothelial cells and human endothelial cells via activation of NF-kappa B, HIF-1 alpha, and AP-1.
Authors: Yeligar Et al.
J Immunol 2009;183:5964
Ethanol-induced expression of ET-1 and ET-BR in liver sinusoidal endothelial cells and human endothelial cells involves hypoxia-inducible factor-1alpha and microrNA-199.
Authors: Yeligar Et al.
J Immunol 2009;183:5232
c-jun controls the ability of IL-12 to induce IL-10 production from human memory CD4+ T cells.
Authors: Garcia Et al.
J Immunol 2009;183:4475
C5a mediates peripheral blood neutrophil dysfunction in critically ill patients.
Authors: Morris Et al.
Am J Respir Crit Care Med 2009;180:19
Soy phytoestrogens are neuroprotective against stroke-like injury in vitro.
Authors: Schreihofer and Redmond
J Neurosci 2009;158:602
Efficacy of signal pathway inhibitors alone and in combination with cisp. varies between human non-small cell lung cancer lines.
Authors: Kilic Et al.
Blockade of estrogen receptor signaling inhibits growth and migration of medulloblastoma.
Authors: Belcher Et al.
Mechanisms underlying fibronectin-induced up-regulation of P2X4R expression in microglia: distinct roles of PI3K-Akt and MEK-ERK signalling pathways.
Authors: Tsuda Et al.
J Cell Mol Med 2009;13:3251
Inulin increases glucose transport in C2C12 myotubes and HepG2 cells via activation of AMP-activated protein kinase and phosphatidylinositol 3-kinase pathways.
Authors: Yun Et al.
PLoS One 2009;12:1023
Synergistic effect of ERK inhibition on tetrandrine-induced apoptosis in A549 human lung carcinoma cells.
Authors: Cho Et al.
J Vet Sci 2009;10:23
PI3 kinase/Akt activation mediates estrogen and IGF-1 nigral DA neuronal neuroprotection against a unilateral rat model of Parkinson's disease.
Authors: Quesada Et al.
Dev Neurobiol 2008;68:632
Reactive oxygen species stabilize hypoxia-inducible factor-1 alpha protein and stimulate transcriptional activity via AMP-activated protein kinase in DU145 human prostate cancer cells.
Authors: Jung Et al.
Phosphatidylinositol 3-kinase is a key mediator of central sensitization in painful inflammatory conditions.
Authors: Pezet Et al.
J Neurosci 2008;28:4261
Temporal profiling of changes in phosphatidylinositol 4,5-bisphosphate, inositol 1,4,5-trisphosphate and diacylglycerol allows comprehensive analysis of phospholipase C-initiated signalling in single neurons.
Authors: Nelson Et al.
J Neurochem 2008;107:602
Hallucinogens recruit specific cortical 5-HT(2A) receptor-mediated signaling pathways to affect behavior.
Authors: González-Maeso Et al.
Exp Mol Med 2007;53:439
Resveratrol stimulates glucose transport in C2C12 myotubes by activating AMP-activated protein kinase.
Authors: Park Et al.
Br J Pharmacol 2007;39:222
cis-9,trans-11-conjugated linoleic acid down-regulates phorbol ester-induced NF-kappaB activation and subsequent COX-2 expression in hairless mouse skin by targeting IkappaB kinase and PI3K-Akt.
Authors: Hwang Et al.
Regulation of DA transporter function and cell surface expression by D3 DA receptors.
Authors: Zapata Et al.
J Biol Chem 2007;282:35842
IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
Authors: Chung Et al.
J Endocrinol 2007;194:77
Ins induces airway smooth muscle contraction.
Authors: Schaafsma Et al.
J Biomed Sci 2007;150:136
PI-3-kinase-dependent membrane recruitment of centaurin-α2 is essential for its effect on ARF6-mediated actin cytoskeleton reorganisation.
Authors: Venkateswarlu Et al.
Cyclin D1 is necessary for tamoxifen-induced cell cycle progression in human breast cancer cells.
Authors: Kilker and Planas-Silva
Mol Immunol 2006;66:11478
Differential reelin-induced enhancement of NMDA and AMPA receptor activity in the adult hippocampus.
Authors: Qiu Et al.
Br J Pharmacol 2006;26:12943
Ischemic preconditioning protects by activating prosurvival kinases at reperfusion.
Authors: Hausenloy Et al.
Am J Physiol Heart Circ Physiol 2005;288:H971
Glucose deprivation increases mRNA stability of vascular endothelial growth factor through activation of AMP-activated protein kinase in DU145 prostate carcinoma.
Authors: Yun Et al.
J Neurosci 2005;280:9963
LY 294002 inhibits adenosine receptor activation by a mechanism independent of effects on PI-3 kinase or casein kinase II.
Authors: Searl and Silinsky
Purinergic Signal 2005;1:389
Phospholipase C-linked receptors regulate the ATP-sensitive potassium channel by means of phosphatidylinositol 4,5-bisphosphate metabolism.
Authors: Xie Et al.
Proc Natl Acad Sci U S A 1999;96:15292
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Reviews for LY 294002 hydrochloride
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BV2 microglia cells were incubated for one hour with 10µM LY294002 prior to treatment with 1µM LPA. Western blot analysis revealed a possible role for PI3K in the LPA induced expression of pAMPK.
Human osteosarcoma cells were incubated with 10 μM LY 294002 for 30 min prior to treatment with 10 μM LPA to estimate COX-2 expression using Western blot analysis. LY 294002 abolished LPA-induced COX-2 expression.
MG-63 cells were incubated with PD169316 (25 μM), LY294002 (10 μM) or Akt-1/2 (5 μM Akt-I) for 30 min prior to 15d-PGJ2 treatment (20 μM) for 1 h to follow pAkt expression using Western blot. Akt-1/2 completely blocked 15d-PGJ2-induced Akt phosphorylation in MG-63 cells.
I used LY294002 hydrochloride 10µM to inhibit pAKT response of FFAR GPCR activators (15min 37°C).
Mouse ovarian theca cells isolated from 60-day old mice were used. Cultured Ptenfl/fl and tPtenMT ovarian theca cells were pretreated with vehicle (DMSO), LY294002 (50 mM), or API-2 (7.5 mM) for 1 h before the addition of LH (50 ng/mL) for 30 min. Western blotting was used to detect Foxo1 phosphorylation in cultured ovarian theca cells.