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505763 ProRS Inhibitor, Halofuginone - CAS 64924-67-0 - Calbiochem

A cell-permeable racemic mixture of Halofuginone that inhibits of prolyl-tRNA synthetase.

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Synonymes: STENOROL, HF, Hydrobromide, prolyl-tRNA synthetase Inhibitor, trans-(±)-7-Bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4(3H)-quinazolinone hydrobromide

Primary Target: prolyl-tRNA synthetase
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505763
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Tableau de caractéristiques principal

CAS #Empirical Formula
64924-67-0C₁₆H₁₇BrClN₃O₃•HBr

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      Description
      OverviewA cell-permeable racemic mixture of Halofuginone whose D-(+)/(2R, 3S) enantiomer serves as the active inhibitor against ProRS-mediated aminoacylation by simultaneously preventing ProRS-catalyzed Pro-AMP formation and the subsequent Pro transfer from Pro-AMP to tRNAPro. Proline, but not other NEAA, is able to reverse the inhibitory effect of HF in in vitro rabbit reticulocyte lysate translations (1 µM HF; 1 mM Pro) and prevent HF-induced cellular AAR pathway activation (100 nM HF/2 mM Pro/MEF; 10 nM HF/1 mM Pro/Murine CD4+ CD25- T cells). Shown to inhibit bFGF-induced neovascularization in a murine corneal angiogenesis model (5 mg/kg/d via food intake) and significantly reduce the severity of MOG33-55-induced EAE in mice (2 µg/mouse/d i.p.) in vivo. Unlike AA-AMP mimetics, HF does not compete against ATP for ProRS binding.
      Catalogue Number505763
      Brand Family Calbiochem®
      SynonymsSTENOROL, HF, Hydrobromide, prolyl-tRNA synthetase Inhibitor, trans-(±)-7-Bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4(3H)-quinazolinone hydrobromide
      References
      ReferencesZhou, H., et al. 2013, Nature 494, 121.
      Keller, T.L., et al. 2012, Nat. Chem. Biol. 12, 311.
      Sundrud, M.S., et al. 2009, Science 324, 1334.
      Elkin, M., et al. 2000, FASEB J. 14, 2477.
      Elkin, M., et al. 1999, Clin. Cancer Res. 5, 1982.
      Product Information
      CAS number64924-67-0
      FormWhite powder
      Hill FormulaC₁₆H₁₇BrClN₃O₃•HBr
      Chemical formulaC₁₆H₁₇BrClN₃O₃•HBr
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetprolyl-tRNA synthetase
      Primary Target IC<sub>50</sub>18 nM
      Purity≥98% 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 at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°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
      Global Trade Item Number
      Référence GTIN
      5057630001 04055977243536

      Documentation

      ProRS Inhibitor, Halofuginone - CAS 64924-67-0 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Zhou, H., et al. 2013, Nature 494, 121.
      Keller, T.L., et al. 2012, Nat. Chem. Biol. 12, 311.
      Sundrud, M.S., et al. 2009, Science 324, 1334.
      Elkin, M., et al. 2000, FASEB J. 14, 2477.
      Elkin, M., et al. 1999, Clin. Cancer Res. 5, 1982.
      Fiche technique

      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-March-2014 JSW
      SynonymsSTENOROL, HF, Hydrobromide, prolyl-tRNA synthetase Inhibitor, trans-(±)-7-Bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4(3H)-quinazolinone hydrobromide
      DescriptionA cell-permeable racemic mixture of Halofuginone, a halogenated derivative of the Dichroa febriguga alkaloid Febrifugine, whose D-(+)/(2R, 3S) enantiomer serves as the active inhibitor against ProRS- (prolyl-tRNA synthetase) mediated aminoacylation by simultaneously targeting/blocking ProRS Proline-binding pocket with its hydroxypiperidine and tRNA 3′ end adenosine-binding site with its halogenated 4-quinazolinone, preventing not only ProRS-catalyzed prolyl adenylation (Pro-AMP formation), but also the subsequent Pro transfer from Pro-AMP to tRNAPro. Consistently, only proline, but not other NEAA, is able to reverse the inhibitory effect of HF in in vitro rabbit reticulocyte lysate translations (1 µM HF; 1 mM Pro) and prevent HF-induced cellular AAR (amino acid response) pathway activation (100 nM HF/2 mM Pro/MEF; 10 nM HF/1 mM Pro/Murine CD4+ CD25- T cells). Shown to inhibit bFGF-induced neovascularization in a murine corneal angiogenesis model (5 mg/kg/day via food intake) and significantly reduce the severity of myelin antigen MOG33-55-induced autoimmune EAE/encephalomyelitis in mice (2 µg/mouse/day i.p.) in vivo. Unlike AA-AMP mimetics, HF does not compete against ATP for ProRS binding. ATP, in its ProRS bound state, actually helps stabilize HF via hydrogen bond interactions.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number64924-67-0
      Chemical formulaC₁₆H₁₇BrClN₃O₃•HBr
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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
      ReferencesZhou, H., et al. 2013, Nature 494, 121.
      Keller, T.L., et al. 2012, Nat. Chem. Biol. 12, 311.
      Sundrud, M.S., et al. 2009, Science 324, 1334.
      Elkin, M., et al. 2000, FASEB J. 14, 2477.
      Elkin, M., et al. 1999, Clin. Cancer Res. 5, 1982.