Replaces Prod. #: ALX-270-038
Potent, cell permeable, inhibitor of PI(3)K (phosphoinositide 3-kinase) that acts on the ATP-binding site of the enzyme. Displays an IC50 of 1.4µM and inhibits all isoforms equally in in vitro assays using purified PI 3-kinase (p110α IC50=0.63µM). Inhibits Pim-1 kinase with IC50=4.0µM. Other kinases such as PKC, PKA, MAP kinase, S6 kinase, EGF receptor tyrosine kinase, c-src kinase, PI 4-kinase, diacylglycerol kinase or rabbit kidney ATPase are not inhibited at 50µM.
Induces apoptosis in many cell types by blocking the PI3-K/Akt anti-apoptotic pathway. Useful tool for identifying cellular events which are regulated by the PI3-K/Akt axis. Sensitizes tumor cells to drug-induced apoptosis independent of its PI3K inhibitory activity. Inhibits proliferation and induces apoptosis in human colon cancer cells. Suppresses proliferation of mouse embryonic stem cells. Furthermore, inhibits autophagic sequestration in rat hepatocytes.
Product Details
| Alternative Name: | 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one |
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| Formula: | C19H17NO3 |
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| MW: | 307.3 |
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| CAS: | 154447-36-6 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | White to pale yellow solid. |
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| Solubility: | Soluble in DMSO (25mg/ml, warm), 100% ethanol (25mg/ml, warm) or methanol. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for at least 1 year after receipt when stored at -20°C. Stock solutions are stable for up to 3 months at -20°C. |
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| Technical Info/Product Notes: | Replacement for ADI-HPK-106. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
YAP Overexpression in Breast Cancer Cells Promotes Angiogenesis through Activating YAP Signaling in Vascular Endothelial Cells: Y. Yan, et al.; Anal. Cell. Pathol. (Amst.)
2022, 5942379 (2022),
Abstract;
Acid sphingomyelinase promotes SGK1-dependent vascular calcification: T. Luong, et al.; Clin. Sci.
135, 515 (2021),
Abstract;
Full Text
Carbon Monoxide Releasing Molecule-3 Enhances Heme Oxygenase-1 Induction via ROS-Dependent FoxO1 and Nrf2 in Brain Astrocytes: C. C. Lin, et al.; Oxid. Med. Cell. Longev.
2021, 5521196 (2021),
Abstract;
Exendin-4, a glucagon-like peptide receptor agonist, facilitates osteoblast differentiation via connexin43: J. Chen, et al.; Endocrine
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Abstract;
LDOC1 Suppresses Microbe-Induced Production of IL-1β in Human Normal and Cancerous Oral Cells through the PI3K/Akt/GSK-3β Axis: C. Lee, et al.; Cancers (Basel)
12, 3148 (2020),
Abstract;
Full Text
Effect of selective serotonin (5-HT)2B receptor agonist BW723C86 on epidermal growth factor/transforming growth factor-α receptor tyrosine kinase and ribosomal p70 S6 kinase activities in primary cultures of adult rat hepatocytes: K. Naito, et al.; Biol. Pharm. Bull.
42, 631 (2019),
Application(s): used w. adult rat liver hepatocytes,
Abstract;
Full Text
SGK1-dependent stimulation of vascular smooth muscle cell osteo-/chondrogenic transdifferentiation by interleukin-18: N. Schelski, et al.; Pflugers Arch.
471, 889 (2019),
Abstract;
Full Text
CCL4 enhances preosteoclast migration and its receptor CCR5 downregulation by RANKL promotes osteoclastogenesis: D. Lee, et al.; Cell Death Dis.
9, 495 (2018),
Abstract;
Full Text
Intracellular formyl peptide receptor regulates naïve CD4 T cell migration: H.Y. Lee, et al.; Biochem. Biophys. Res. Commun.
497, 226 (2018),
Abstract;
16-Hydroxycleroda-3, 13-dien-15, 16-olide inhibits the proliferation and induces mitochondrial-dependent apoptosis through Akt, mTOR, and MEK-ERK pathways in human renal carcinoma cells: C. Liu, et al.; Phytomedicine
36, 95 (2017),
Abstract;
Anti-neoplastic drugs increase caveolin-1-dependent migration, invasion and metastasis of cancer cells: N.I. Díaz-Valdivia, et al.; Oncotarget
8, 111943 (2017),
Abstract;
Full Text
Involvement of PI3K and PKA pathways in mouse tongue epithelial differentiation: J.K. Jung, et al.; Acta Histochem.
119, 92 (2017),
Abstract;
AMPK activates LXRα and ABCA1 expression in human macrophages: M. Kemmerer, et al.; Int. J. Biochem. Cell Biol.
16, 30154 (2016),
Application(s): Cell culture using human monocytic cells,
Abstract;
Co-treatment of LY294002 or MK-2206 with AZD5363 Attenuates AZD5363-induced Increase in the Level of Phosphorylated AKT: A.R. Choi, et al.; Anticancer Res.
36, 5849 (2016),
Application(s): Cell treatment, MK-2206 cells,
Abstract;
Full Text
Antigen receptor-mediated depletion of FOXP3 in induced regulatory T-lymphocytes via PTPN2 and FOXO1: E. Bothur, et al.; Nat. Commun.
6, 8576 (2015),
Application(s): Cell preparation and in vitro stimulation,
Abstract;
Full Text
Corticotropin-Releasing Hormone (CRH) Promotes Macrophage Foam Cell Formation via Reduced Expression of ATP Binding Cassette Transporter-1 (ABCA1): W. Cho, et al.; PLoS One
10, e0130587 (2015),
Application(s): Cell Culture,
Abstract;
Full Text
Yersinia entry into host cells requires Rab5-dependent dephosphorylation of PI(4,5)P₂ and membrane scission: H. Sarantis, et al.; Cell Host Microbe
11, 117 (2015),
Application(s): COS cells treatment,
Abstract;
Full Text
Zinc Oxide Nanoparticles Induce Lipoxygenase-mediated Apoptosis and Necrosis in Human Neuroblastoma SH-SY5Y Cells: J.H. Kim, et al.; Neurochem. Int.
90, 204 (2015),
Application(s): Cell Culture,
Abstract;
Acidic preconditioning improves the proangiogenic responses of endothelial colony forming cells: H.A. Mena, et al.; Angiogenesis
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Abstract;
Insulin suppresses IKs (KCNQ1/KCNE1) currents, which require β-subunit KCNE1: M. Wu, et al.; Pflugers Arch.
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Abstract;
Lack of Liver X Receptors Leads to Cell Proliferation in a Model of Mouse Dorsal Prostate Epithelial Cell: J. Dufour, et al.; PLoS One
8, e58876 (2013),
Abstract;
Full Text
Novel insulin sensitizer modulates nutrient sensing pathways and maintains β-cell phenotype in human islets: N. Rohatgi, et al.; PloS One
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Application(s): WB, PCR, IHC,
Abstract;
Full Text
Fyn is induced by Ras/PI3K/Akt signaling and is required for enhanced invasion/migration: V. Yadav; Mol. Carcinog.
50, 346 (2011),
Application(s): WB, PCR,
Abstract;
Full Text
Early activation of the beta-catenin pathway in osteocytes is mediated by nitric oxide, phosphatidyl inositol-3 kinase/Akt, and focal adhesion kinase: A. Santos, et al.; Biochem. Biophys. Res. Commun.
391, 364 (2010),
Application(s): WB, PCR, PFF,
Abstract;
mRNA degradation plays a significant role in the program of gene expression regulated by phosphatidylinositol 3-kinase signaling: J.R. Graham, et al.; Mol. Cell. Biol.
30, 5295 (2010),
Application(s): WB, PCR,
Abstract;
Full Text
Sevoflurane postconditioning prevents activation of caspase 3 and 9 through antiapoptotic signaling after myocardial ischemia-reperfusion: Y. Inamura, et al.; J. Anesth.
24, 215 (2010),
Application(s): WB,
Abstract;
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors: M. Hayakawa, et al.; Bioorg. Med. Chem.
15, 5837 (2007),
Abstract;
LY294002 and LY303511 Sensitize Tumor Cells to Drug-Induced Apoptosis via Intracellular Hydrogen Peroxide Production Independent of the Phosphoinositide 3-Kinase-Akt Pathway: T.W. Poh and S. Pervaiz; Cancer Res.
65, 6264 (2005),
Abstract;
Pim-1 Ligand-bound Structures Reveal the Mechanism of Serine/Threonine Kinase Inhibition by LY294002: M.D. Jacobs, et al.; J. Biol. Chem.
280, 13728 (2005),
Abstract;
Investigation of neutrophil signal transduction using a specific inhibitor of phosphatidylinositol 3-kinase: C.J. Vlahos, et al.; J. Immunol.
154, 2413 (1995),
Abstract;
Phosphoinositide 3-kinase inhibition spares actin assembly in activating platelets but reverses platelet aggregation: T.J. Kovacsovics, et al.; J. Biol. Chem.
270, 11358 (1995),
Abstract;
Full Text
Requirement for phosphatidylinositol-3 kinase in the prevention of apoptosis by nerve growth factor: R. Yao & G.M. Cooper; Science
267, 2003 (1995),
Abstract;
A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4- morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002): C.J. Vlahos, et al.; J. Biol. Chem.
269, 5241 (1994),
Abstract;
Full Text
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