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440202 LY 294002 - CAS 154447-36-6 - Calbiochem

LY294002, CAS 154447-36-6, is a cell-permeable, potent, reversible, and specific inhibitor of PI 3-kinase ((IC₅₀ = 1.4 µM). Acts on the ATP-binding site.

LY 294002 - CAS 154447-36-6 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one, BRD2 Inhibitor IV, BRD3 Inhibitor III, BRD4 Inhibitor IV

Primary Target: Phosphatidylinositol 3-kinase
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440202
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
154447-36-6C₁₉H₁₇NO₃

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      Description
      OverviewA cell-permeable, potent, reversible and specific phosphatidylinositol 3-kinase inhibitor (IC50 = 1.4 µM) that acts on the ATP-binding site of the enzyme. Also inhibits nonhomologous DNA end-joining (NHEJ) activity of the 460 kDa phosphatidylinositol 3-like kinase DNA-PKcs, which is the catalytic subunit of DNA-activated protein kinase. Does not affect the activities of EGF receptor kinase, MAP kinase, PKC, Pl 4-kinase, S6 kinase, and c-Src even at 50 µM. Promotes the nuclear accumulation of active GSK-3b. Reported to suppress the proliferation of murine embryonic stem cells. Blocks the proliferation of cultured rabbit aortic smooth muscle cells without inducing apoptosis. Shown to bind to the same site as I-BET (Cat. No. 40101050 ~ 10 µM). A 10 mM (1 mg/325 µl) solution of LY 294002 (Cat. No. 440204) in DMSO is also available.
      Catalogue Number440202
      Brand Family Calbiochem®
      Synonyms2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one, BRD2 Inhibitor IV, BRD3 Inhibitor III, BRD4 Inhibitor IV
      References
      ReferencesDittman, A., et al. 2013. ACS Chem. Biol. 9, 495.
      Bechard, M., and Dalton. S. 2009. Mol. Cell. Biol. 29, 2092.
      Lianguzova, M.S. et al. 2007. Cell Biol. Int. 31, 330.
      Baumann, P., and West, S.C. 1998. Proc. Natl. Acad. Sci. USA 95, 14066.
      Cardone, M.H., et al. 1998. Science 282, 1318.
      Vlahos, C.J., et al. 1995. J. Immunol. 154, 2413.
      Yano, H., et al. 1995. Biochem. J. 312, 145.
      Vlahos, C.J., et al. 1994. J. Biol. Chem. 269, 5241.



      Selected Citations
      Lee, J., et al. 2009. Cell Stem Cell 5, 76.
      Product Information
      CAS number154447-36-6
      ATP CompetitiveY
      FormOff-white solid
      Hill FormulaC₁₉H₁₇NO₃
      Chemical formulaC₁₉H₁₇NO₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPhosphatidylinositol 3-kinase
      Primary Target IC<sub>50</sub>1.4 µM against phosphatidylinositol 3-kinase
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      440202-5MGCN 07790788050290

      Documentation

      LY 294002 - CAS 154447-36-6 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      LY 294002 - CAS 154447-36-6 - Calbiochem Certificates of Analysis

      TitleLot Number
      440202

      References

      Reference overview
      Dittman, A., et al. 2013. ACS Chem. Biol. 9, 495.
      Bechard, M., and Dalton. S. 2009. Mol. Cell. Biol. 29, 2092.
      Lianguzova, M.S. et al. 2007. Cell Biol. Int. 31, 330.
      Baumann, P., and West, S.C. 1998. Proc. Natl. Acad. Sci. USA 95, 14066.
      Cardone, M.H., et al. 1998. Science 282, 1318.
      Vlahos, C.J., et al. 1995. J. Immunol. 154, 2413.
      Yano, H., et al. 1995. Biochem. J. 312, 145.
      Vlahos, C.J., et al. 1994. J. Biol. Chem. 269, 5241.



      Selected Citations
      Lee, J., et al. 2009. Cell Stem Cell 5, 76.

      Brochure

      Title
      An Introduction to Inhibitors and Their Biological Applications - 1st Edition
      Bulk Product Guide

      Technical Info

      Title
      JAK/STAT Signaling Research Focus

      Data Sheet

      Title
      Reprogramming Cell Fate and Function Novel Strategies for iPSC Generation, Characterization, and Differentiation

      Posters

      Title
      Human Kinome & InhibitorSelect™ Libraries

      Citations

      Title
    • Bechard, M., and Dalton. S. 2009. Mol. Cell. Biol. 29, 2092.
    • Lianguzova, M.S. et al. 2007. Cell Biol. Int. 31, 330.
    • Oliveira, J.B., et al. 2007. Procedings of the National Academy of Science 104, 8953.
    • Satoshi Fukumoto, et al. (2006) Laminin 5 is required for dental epithelium growth and polarity and the development of tooth bud and shape. Journal of Biological Chemistry 281, 5008-5016.
    • Ana Olivera, et al. (2006) IgE-dependent activation of sphingosine kinase 1 and 2 and secretion of sphingosine-1-phosphate requires Fyn kinase and contributes to mast cell responses. Journal of Biological Chemistry 281, 2515-2525.
    • Qian Yang, et al. (2006) TSC1/TSC2 and Rheb have different effects on TORC1 and TORC2 activity. Proceedings of the National Academy of Sciences (USA) 103, 6811-6816.
    • Ying Zhang, Mingjuan Liao and Maria L. Dufau. (2006) Phosphatidylinositol 3-kinase/protein kinase Cγ-induced phosphorylation of Sp1 and p107 repressor release have a critical role in histone deacetylase inhibitor-mediated depression of transcription of the luteinizing hormone receptor gene. Molecular and Cellular Biology 26, 6748-6761.
    • Huanyu Dou, et al. (2005) Neuroprotective mechanisms of lithium in murine human immunodeficiency virus-1 encephalitis. Journal of Neuroscience 25, 8375-8385.
    • Julie Lotharius, et al. (2005) Progressive degeneration of human mesencephalic neuron-derived cells triggered by dopamine-dependent oxidative stress is dependent on the mixed lineage kinase pathway. Journal of Neuroscience 25, 6329-6342.
    • Meenalakshmi M. Mariappan, M.M., et al. (2005) Phospholipase Cγ-Erk Axis in Vascular Endothelial Growth Factor-Induced Eukaryotic Initiation Factor 4E Phosphorylation and Protein Synthesis in Renal Epithelial Cells. Journal of Biological Chemistry 280, 28402-28411.
    • Michael Tscharntke, et al. (2005) Ras-induced spreading and wound closure in human epidermal keratinocytes. The FASEB Journal in press,.
    • Junji Tsurutani, et al. (2005) Inhibition of the phosphatidylinositol 3-kinase/Akt/Mammalian target of rapamycin pathway but no the MEK/ERK Pathway attentuates laminin-meidated small cell lunch cancer cellular survival and resistance to Imatinib mesylate or chemolyte.. Cancer Research 65, 8423-8432.
    • Xinbo Liao, et al. (2003) Androgen stimulates matrix metalloproteinase-2 expression in human prostate cancer. Endocrinology 144, 1656-1663.
      		•
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision28-February-2012 RFH
      Synonyms2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one, BRD2 Inhibitor IV, BRD3 Inhibitor III, BRD4 Inhibitor IV
      DescriptionA cell-permeable, potent, reversible, and specific phosphatidylinositol 3-kinase (PI 3-kinase) inhibitor that acts on the ATP-binding site of the enzyme (IC50 = 1.4 µM). Also inhibits nonhomologous DNA end-joining (NHED) in the 460 kDa phosphatidylinositol 3-like kinase DNA-PKcs, which is the catalytic subunit of DNA-activated protein kinase. Does not affect the activity of EGF receptor kinase, MAP kinase, PKC, PI 4-kinase, S6 kinase, and c-src at 50 µM. Promotes the nuclear accumulation of active GSK-3b. Reported to suppress the proliferation of murine embryonic stem cells. Blocks the proliferation of cultured rabbit aortic smooth muscle cells without inducing apoptosis. Reported to inhibit histamine secretion in RBL-2H3 cells (IC50 = 5 µM).
      FormOff-white solid
      CAS number154447-36-6
      Chemical formulaC₁₉H₁₇NO₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (20 mg/ml) or Ethanol. Slight warming may be required to achieve complete solubilization.
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesDittman, A., et al. 2013. ACS Chem. Biol. 9, 495.
      Bechard, M., and Dalton. S. 2009. Mol. Cell. Biol. 29, 2092.
      Lianguzova, M.S. et al. 2007. Cell Biol. Int. 31, 330.
      Baumann, P., and West, S.C. 1998. Proc. Natl. Acad. Sci. USA 95, 14066.
      Cardone, M.H., et al. 1998. Science 282, 1318.
      Vlahos, C.J., et al. 1995. J. Immunol. 154, 2413.
      Yano, H., et al. 1995. Biochem. J. 312, 145.
      Vlahos, C.J., et al. 1994. J. Biol. Chem. 269, 5241.



      Selected Citations
      Lee, J., et al. 2009. Cell Stem Cell 5, 76.
      Citation
    • Bechard, M., and Dalton. S. 2009. Mol. Cell. Biol. 29, 2092.
    • Lianguzova, M.S. et al. 2007. Cell Biol. Int. 31, 330.
    • Oliveira, J.B., et al. 2007. Procedings of the National Academy of Science 104, 8953.
    • Satoshi Fukumoto, et al. (2006) Laminin 5 is required for dental epithelium growth and polarity and the development of tooth bud and shape. Journal of Biological Chemistry 281, 5008-5016.
    • Ana Olivera, et al. (2006) IgE-dependent activation of sphingosine kinase 1 and 2 and secretion of sphingosine-1-phosphate requires Fyn kinase and contributes to mast cell responses. Journal of Biological Chemistry 281, 2515-2525.
    • Qian Yang, et al. (2006) TSC1/TSC2 and Rheb have different effects on TORC1 and TORC2 activity. Proceedings of the National Academy of Sciences (USA) 103, 6811-6816.
    • Ying Zhang, Mingjuan Liao and Maria L. Dufau. (2006) Phosphatidylinositol 3-kinase/protein kinase Cγ-induced phosphorylation of Sp1 and p107 repressor release have a critical role in histone deacetylase inhibitor-mediated depression of transcription of the luteinizing hormone receptor gene. Molecular and Cellular Biology 26, 6748-6761.
    • Huanyu Dou, et al. (2005) Neuroprotective mechanisms of lithium in murine human immunodeficiency virus-1 encephalitis. Journal of Neuroscience 25, 8375-8385.
    • Julie Lotharius, et al. (2005) Progressive degeneration of human mesencephalic neuron-derived cells triggered by dopamine-dependent oxidative stress is dependent on the mixed lineage kinase pathway. Journal of Neuroscience 25, 6329-6342.
    • Meenalakshmi M. Mariappan, M.M., et al. (2005) Phospholipase Cγ-Erk Axis in Vascular Endothelial Growth Factor-Induced Eukaryotic Initiation Factor 4E Phosphorylation and Protein Synthesis in Renal Epithelial Cells. Journal of Biological Chemistry 280, 28402-28411.
    • Michael Tscharntke, et al. (2005) Ras-induced spreading and wound closure in human epidermal keratinocytes. The FASEB Journal in press,.
    • Junji Tsurutani, et al. (2005) Inhibition of the phosphatidylinositol 3-kinase/Akt/Mammalian target of rapamycin pathway but no the MEK/ERK Pathway attentuates laminin-meidated small cell lunch cancer cellular survival and resistance to Imatinib mesylate or chemolyte.. Cancer Research 65, 8423-8432.
    • Xinbo Liao, et al. (2003) Androgen stimulates matrix metalloproteinase-2 expression in human prostate cancer. Endocrinology 144, 1656-1663.
      		•