475988 mTOR Inhibitor III, PP242 - Calbiochem

475988
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Overview

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Key Spec Table

Empirical Formula
C₁₆H₁₆N₆O • 2H₂O

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475988-5MGCN
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      5 mg
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      Description
      OverviewA cell-permeable pyrazolopyrimidine compound that acts as a potent, reversible, and ATP-competitive inhibitor against both mTORC1 & mTORC2 (IC50 = 30 & 58 nM, respectively, with 100 µM ATP). PP242 inhibits PKCα, p110γ, and JAK2 with 6-, 13-, and 14-fold less potency and exhibits much reduced or no activity against a panel of 216 other kinases at a concentration of 1 µM (maximum of 68% or 77% inhibition observed with 10 or 100 µM ATP, respectively). PP242 differentially inhibits insulin-stimulated phosphorylations of cellular proteins both in cultures (2.5 µM) in vitro and in mice (20 mg/kg i.p.) in vivo in a manner distinctly different from that seen in mTORC2-functional knockout SIN1-/- cells or in cultures treated with Rapamycin (Cat. Nos. 553210, 553211, 553212), which targets only mTORC1, but not mTORC2. Blockage of 4EBP1 T36/T45/S65 phosphorylation by PP242 upon insulin stimulation in primary MEFs correlates well with an enhanced 4EBP1 association with the cap-binding protein eIF4E, resulting in a selective inhibition of cap-dependent, but not cap-independent, protein translation.
      Catalogue Number475988
      Brand Family Calbiochem®
      Synonyms2-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol, Dihydrate, TORKinib, mTOR Inhibitor III, PP242
      References
      ReferencesFeldman, M.E., et al. 2009. PLoS Biology 7, 391.
      Apsel, B., et al. 2008. Nat. Chem. Biol. 4, 691.
      Product Information
      FormOff-white solid
      Hill FormulaC₁₆H₁₆N₆O • 2H₂O
      Chemical formulaC₁₆H₁₆N₆O • 2H₂O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped with Blue Ice or with Dry Ice
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      mTOR Inhibitor III, PP242 - Calbiochem Certificates of Analysis

      TitleLot Number
      475988

      References

      Reference overview
      Feldman, M.E., et al. 2009. PLoS Biology 7, 391.
      Apsel, B., et al. 2008. Nat. Chem. Biol. 4, 691.
      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.

      Revision31-May-2012 JSW
      Synonyms2-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol, Dihydrate, TORKinib, mTOR Inhibitor III, PP242
      DescriptionA cell-permeable pyrazolopyrimidine compound that acts as a potent, reversible, and ATP-competitive inhibitor against both mTORC1 & mTORC2 (IC50 = 30 & 58 nM, respectively, with 100 µM ATP). PP242 inhibits PKCα, p110γ, and JAK2 with 6-, 13-, and 14-fold less potency and exhibits much reduced or no activity against a panel of 216 other kinases at a concentration of 1 µM (maximum of 68% or 77% inhibition observed with 10 or 100 µM ATP, respectively). PP242 differentially inhibits insulin-stimulated phosphorylations of cellular proteins both in cultures (2.5 µM) in vitro and in mice (20 mg/kg i.p.) in vivo in a manner distinctly different from that seen in mTORC2-functional knockout SIN1-/- cells or in cultures treated with Rapamycin (Cat. Nos. 553210, 553211, 553212), which targets only mTORC1, but not mTORC2. Blockage of 4EBP1 T36/T45/S65 phosphorylation by PP242 upon insulin stimulation in primary MEFs correlates well with an enhanced 4EBP1 association with the cap-binding protein eIF4E, resulting in a selective inhibition of cap-dependent, but not cap-independent, protein translation.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₆H₁₆N₆O • 2H₂O
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage -20°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesFeldman, M.E., et al. 2009. PLoS Biology 7, 391.
      Apsel, B., et al. 2008. Nat. Chem. Biol. 4, 691.