Prototypical PI 3-kinase inhibitor (IC
values are 0.31, 0.73, 1.06 and 6.60
M for PI 3-K
, PI 3-K
, PI 3-K
and PI 3-K
respectively). Also inhibits other kinases including, CK2, mTOR, PLK1, PIM1 and PIM3. Inhibits proliferation and induces apoptosis in human colon cancer cells
. Suppresses proliferation of mESCs. Inhibits autophagic sequestration in rat hepatocytes.
Negative Control also available. View R&D Systems' research poster featuring LY 294002 hydrochloride.
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All Tocris products are intended for laboratory research use only.
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The citations listed below are publications that use Tocris products.
Selected citations for LY 294002 hydrochloride include:
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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 formoterol but not clenbuterol.
Sci Rep 2017;7(1):10578
Signaling Cascade Involved in Rapid Stimulation of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by Dexamethasone.
Authors: Bossmann Et al.
Int J Mol Sci 2017;18
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.
B positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cellslacking functional GABA B 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
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
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
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 insulin 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
Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-dopamine-like G protein-coupled receptor.
Authors: Bayliss and Evans
PLoS One 2013;8:e80833
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
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
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-Estradiol 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
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 insulin-like growth factor (IGF) I receptor sensitivity to Ambient IGF, leading to phosphatidylinositol 3-kinase/AKT-dependent Wnt/LRP5 recept
Authors: Sunters Et al.
J Biol Chem 2010;285:8743
miR-155 and its star-form partner miR-155* cooperatively regulate type I interferon 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
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 hyperdopamine 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 Cisplatin 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 dopamine transporter function and cell surface expression by D3 dopamine 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
Insulin 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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