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

Overview

Key Spec Table

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
      Biological Information
      Primary Targetprolyl-tRNA synthetase
      Primary Target IC<sub>50</sub>18 nM
      Purity≥98% by HPLC
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5.05763.0001 04055977243536