LY 294002 hydrochloride

Cat. No. 1130

LY 294002 hydrochloride C19H17NO3.HCl [934389-88-5]

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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 LY 303511 (Cat. No. 2418) also available.

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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

Bain et al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297. PMID: 17850214.

Lianguzova et al (2007) Phosphoinositide 3-kinase inhibitor LY294002 but not serum withdrawal suppresses proliferation of murine embryonic stem cells. Cell Biol.Int. 31 330. PMID: 17321171.

Blommaart et al (1997) The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes. Eur.J.Biochem. 243 240. PMID: 9030745.

Vlahos et al (1994) A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY 294002). J.Biol.Chem. 269 5241. PMID: 8106507.

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Citations are publications that use Tocris products. Selected citations for LY 294002 hydrochloride include:

Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell 19 217. PMID: 27320041.

Shao-Hua Su et al (2016) 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 Behavioural Brain Research 313 334. PMID: 27424778.

Laube et al (2015) Glucocorticoids Distinctively Modulate the CFTR Channel with Possible Implications in Lung Development and Transition into Extrauterine Life. PLoS One 10 e0124833. PMID: 25910246.

Markus et al (2015) An in vitro model of latency and reactivation of varicella zoster virus in human stem cell-derived neurons. PLoS Pathog 11 e1004885. PMID: 26042814.

Dai et al (2014) Interaction of mTOR and Erk1/2 signaling to regulate oligodendrocyte differentiation. Glia 62 2096. PMID: 25060812.

Gonsalves et al (2014) Angiogenic growth factors augment K-Cl cotransporter expression in erythroid cells via hypoxia-inducible factor-1α. Am J Hematol 89 273. PMID: 24227191.

Kim et al (2014) Decrease of PKB/Akt Phosphorylation is Partially Mediated by SAPK/JNK Activation in Serum-free L6 Myoblasts Starved with Low Glucose. J Phys Ther Sci 26 1757. PMID: 25435694.

Mattes et al (2014) Rapid elevation of sodium transport through insulin is mediated by AKT in alveolar cells. Physiol Rep 2 e00269. PMID: 24760523.

Bayliss and Evans (2013) Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-dopamine-like G protein-coupled receptor. PLoS One 8 e80833. PMID: 24265838.

Gangoiti et al (2012) Ceramide 1-phosphate stimulates proliferation of C2C12 myoblasts. Biochimie 94 597. PMID: 21945811.

Lee et al (2012) Fucoidan from seaweed Fucus vesiculosus inhibits migration and invasion of human lung cancer cell via PI3K-Akt-mTOR pathways. PLoS One 7 e50624. PMID: 23226337.

Barrio et al (2011) Neurotoxicity induced by okadaic acid in the human neuroblastoma SH-SY5Y line can be differentially prevented by α7 and β2* nicotinic stimulation. Toxicol Sci 123 193. PMID: 21715663.

Mincheva et al (2011) The canonical nuclear factor-κB pathway regulates cell survival in a developmental model of spinal cord motoneurons. J Neurosci 31 6493. PMID: 21525290.

Moult et al (2010) Leptin regulates AMPA receptor trafficking via PTEN inhibition. J Neurosci 30 4088. PMID: 20237279.

Sunters et al (2010) 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 receptor-independent activation of beta-catenin signaling. J Biol Chem 285 8743. PMID: 20042609.

Zhou et al (2010) miR-155 and its star-form partner miR-155* cooperatively regulate type I interferon production by human plasmacytoid dendritic cells. Blood 116 5885. PMID: 20852130.

Garcia et al (2009) c-jun controls the ability of IL-12 to induce IL-10 production from human memory CD4+ T cells. J Immunol 183 4475. PMID: 19734233.

Morris et al (2009) C5a mediates peripheral blood neutrophil dysfunction in critically ill patients. Am J Respir Crit Care Med 180 19. PMID: 19324972.

Solyakov et al (2009) Regulation of p53 expression, phosphorylation and subcellular localization by a G-protein-coupled receptor. Oncogene 28 3619. PMID: 19648965.

Tsuda et al (2009) Mechanisms underlying fibronectin-induced up-regulation of P2X4R expression in microglia: distinct roles of PI3K-Akt and MEK-ERK signalling pathways. J Cell Mol Med 13 3251. PMID: 19298529.

Wang et al (2009) Glycogen synthase kinase-3 and Omi/HtrA2 induce annexin A2 cleavage followed by cell cycle inhibition and apoptosis. Mol Biol Cell 20 4153. PMID: 19656851.

Yeligar et al (2009) 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. J Immunol 183 5232. PMID: 19783678.

Yeligar et al (2009) 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. J Immunol 183 5964. PMID: 19828633.

Jung et al (2008) 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. Carcinogenesis 29 713. PMID: 18258605.

Nelson et al (2008) 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. J Neurochem 107 602. PMID: 18665913.

Pezet et al (2008) Phosphatidylinositol 3-kinase is a key mediator of central sensitization in painful inflammatory conditions. J Neurosci 28 4261. PMID: 18417706.

Chung et al (2007) IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4. J Endocrinol 194 77. PMID: 17592023.

Hwang et al (2007) 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. Carcinogenesis 28 363. PMID: 16950795.

Zapata et al (2007) Regulation of dopamine transporter function and cell surface expression by D3 dopamine receptors. J Biol Chem 282 35842. PMID: 17923483.

Searl and Silinsky (2005) LY 294002 inhibits adenosine receptor activation by a mechanism independent of effects on PI-3 kinase or casein kinase II. Purinergic Signal 1 389. PMID: 18404524.

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Keywords: LY 294002 hydrochloride, supplier, PI, 3-kinase, inhibitors, inhibits, 3-Kinase, PI3K, Akt, Signaling, Signalling, Phosphoinositide, Kinases, PIP2, Inositol, Lipids, cAMP, LY294002, hydrochloride, prototypical, CK2, mTOR, PLK1, PIM1, PIM3, Tocris Bioscience, PI 3-kinase Inhibitor products

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