Catalog Number: 1130
Chemical Name: 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one hydrochloride
Biological Activity
Prototypical 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. View R&D Systems' research poster featuring LY 294002 hydrochloride.

Technical Data
  • M.Wt:
    343.81
  • Formula:
    C19H17NO3.HCl
  • Solubility:
    Soluble to 25 mM in DMSO and to 5 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    934389-88-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Other Product-Specific Information:
Background References
  1. 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
  2. The selectivity of protein kinase inhibitors: a further update.
    Bain et al.
    Biochem.J., 2007;408:297
  3. The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes.
    Blommaart et al.
    Eur.J.Biochem., 1997;243:240
  4. A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY 294002).
    Vlahos et al.
    J.Biol.Chem., 1994;269:5241
Citations:

The citations listed below are publications that use Tocris products. Selected citations for LY 294002 hydrochloride include:

60 Citations: Showing 1 - 10
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  1. miR-382 targeting PTEN-Akt axis promotes liver regeneration.
    Authors: Bei Et al.
    Elife 2016;7:1584
  2. 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
  3. 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
  4. Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
    Authors: Mou Et al.
    Cell: Stem Cell 2016;19:217
  5. 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
  6. 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
  7. Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo.
    Authors: Najm Et al.
    Int J Cancer 2015;522:216
  8. Integrated β-catenin, BMP, PTEN, and Notch signalling patterns the nephron.
    Authors: Lindström Et al.
    J Biomed Sci 2015;3:e04000
  9. 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
  10. 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.
    Nature 2015;22:106
  11. A novel mechanism for cytoprotection against hypoxic injury: δ-opioid receptor-mediated increase in Nrf2 translocation.
    Authors: Cao Et al.
    Oncotarget 2015;172:1869
  12. 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
  13. 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
  14. 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
  15. 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
  16. ER-α36-mediated rapid estrogen signaling positively regulates ER-positive breast cancer stem/progenitor cells.
    Authors: Deng Et al.
    BMC Cancer 2014;9:e88034
  17. 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
  18. Interaction of mTOR and Erk1/2 signaling to regulate oligodendrocyte differentiation.
    Authors: Dai Et al.
    Glia 2014;62:2096
  19. Rapid elevation of sodium transport through insulin is mediated by AKT in alveolar cells.
    Authors: Mattes Et al.
    Physiol Rep 2014;2:e00269
  20. 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
  21. δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
    Authors: Liang Et al.
    J Exp Bot 2014;171:5417
  22. Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-dopamine-like G protein-coupled receptor.
    Authors: Bayliss and Evans
    PLoS One 2013;8:e80833
  23. ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change.
    Authors: Montané and Menand
    Neuroscience 2013;64:4361
  24. 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
  25. Ceramide 1-phosphate stimulates proliferation of C2C12 myoblasts.
    Authors: Gangoiti Et al.
    Biochimie 2012;94:597
  26. 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
  27. Nucleus accumbens mGluR5-associated signaling regulates binge alcohol drinking under drinking-in-the-dark procedures.
    Authors: Cozzoli Et al.
    Cancer Res 2012;36:1623
  28. 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
  29. 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
  30. 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
  31. 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
  32. Leptin regulates AMPA receptor trafficking via PTEN inhibition.
    Authors: Moult Et al.
    J Neurosci 2010;30:4088
  33. 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
  34. miR-155 and its star-form partner miR-155* cooperatively regulate type I interferon production by human plasmacytoid dendritic cells.
    Authors: Zhou Et al.
    Blood 2010;116:5885
  35. 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
  36. 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
  37. 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
  38. Regulation of p53 expression, phosphorylation and subcellular localization by a G-protein-coupled receptor.
    Authors: Solyakov Et al.
    Oncogene 2009;28:3619
  39. 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
  40. 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
  41. 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
  42. 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
  43. C5a mediates peripheral blood neutrophil dysfunction in critically ill patients.
    Authors: Morris Et al.
    Am J Respir Crit Care Med 2009;180:19
  44. Soy phytoestrogens are neuroprotective against stroke-like injury in vitro.
    Authors: Schreihofer and Redmond
    J Neurosci 2009;158:602
  45. 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
  46. 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
  47. 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.
    Carcinogenesis 2008;29:713
  48. Phosphatidylinositol 3-kinase is a key mediator of central sensitization in painful inflammatory conditions.
    Authors: Pezet Et al.
    J Neurosci 2008;28:4261
  49. 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
  50. 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
  51. Resveratrol stimulates glucose transport in C2C12 myotubes by activating AMP-activated protein kinase.
    Authors: Park Et al.
    Br J Pharmacol 2007;39:222
  52. 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.
    Carcinogenesis 2007;28:363
  53. Regulation of dopamine transporter function and cell surface expression by D3 dopamine receptors.
    Authors: Zapata Et al.
    J Biol Chem 2007;282:35842
  54. IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
    Authors: Chung Et al.
    J Endocrinol 2007;194:77
  55. Insulin induces airway smooth muscle contraction.
    Authors: Schaafsma Et al.
    J Biomed Sci 2007;150:136
  56. PI-3-kinase-dependent membrane recruitment of centaurin-α2 is essential for its effect on ARF6-mediated actin cytoskeleton reorganisation.
    Authors: Venkateswarlu Et al.
    Neuron 2007;120:792
  57. 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
  58. Differential reelin-induced enhancement of NMDA and AMPA receptor activity in the adult hippocampus.
    Authors: Qiu Et al.
    Br J Pharmacol 2006;26:12943
  59. 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
  60. 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
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