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345883 GGTI-298 - CAS 180977-44-0 - Calbiochem

345883
  
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      Overview

      Replacement Information

      Key Specifications Table

      CAS #Empirical Formula
      180977-44-0C₂7H₃3N₃O₃S
      Description
      OverviewA cell-permeable, prodrug form of the GGTase I inhibitor GGTI-297 (Cat. No. 345882). Inhibits the processing of Rap 1A (IC50 = 3 µM) but has no effect on the processing of H-Ras even at concentrations of 15 µM. Inhibits PDGF-receptor tyrosine phosphorylation. Also arrests cells in the G0/G1 phase of the cell cycle, induces apoptosis, and enhances iNOS induction by IL-1β.
      Catalogue Number345883
      Brand Family Calbiochem®
      SynonymsN-4-[2(R)-Amino-3-mercaptopropyl]amino-2-naphthylbenzoyl-(L)-Leucine methyl ester, TFA
      References
      ReferencesQian, Y., et al. 1998. Bioorg. Med. Chem. 6, 293.
      Finder, J.D., et al. 1997. J. Biol. Chem. 272, 13484.
      Miquel, K., et al. 1997. Cancer Res. 57, 1846.
      Vogt, A., et al. 1997. J. Biol. Chem. 272, 27224.
      McGuire, T., et al. 1996. J. Biol. Chem. 271, 27402.
      Vogt, A., et al. 1996. Oncogene 13, 1991.
      Product Information
      CAS number180977-44-0
      ATP CompetitiveN
      FormWhite solid
      FormulationSupplied as a trifluoroacetate salt.
      Hill FormulaC₂7H₃3N₃O₃S
      Chemical formulaC₂7H₃3N₃O₃S
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetRap1a
      Primary Target IC<sub>50</sub>3 µM against processing of Rap 1A
      Purity≥90% 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
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Unstable in solution; reconstitute just prior to use.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalog Number GTIN
      345883 0

      Documentation

      GGTI-298 - CAS 180977-44-0 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      GGTI-298 - CAS 180977-44-0 - Calbiochem Certificates of Analysis

      TitleLot Number
      345883

      References

      Reference overview
      Qian, Y., et al. 1998. Bioorg. Med. Chem. 6, 293.
      Finder, J.D., et al. 1997. J. Biol. Chem. 272, 13484.
      Miquel, K., et al. 1997. Cancer Res. 57, 1846.
      Vogt, A., et al. 1997. J. Biol. Chem. 272, 27224.
      McGuire, T., et al. 1996. J. Biol. Chem. 271, 27402.
      Vogt, A., et al. 1996. Oncogene 13, 1991.

      Citations

      Title
    • Niels W.C.J. van de Donk, et al. (2005) Geranylgeranylated proteins are involved in the regulation of myeloma cell growth. Clinical Cancer Research 11, 429-439.
    • 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.

      Revision10-December-2012 JSW
      SynonymsN-4-[2(R)-Amino-3-mercaptopropyl]amino-2-naphthylbenzoyl-(L)-Leucine methyl ester, TFA
      DescriptionA cell-permeable, prodrug form of the GGTase I inhibitor GGTI-297 (Cat. No. 345882). Inhibits the processing of Rap 1A (IC50 = 3 µM) but had no effect on the processing of H-Ras even at concentrations of 15 µM. Also arrests cells in the G0/G1 phase of the cell cycle, induces apoptosis and enhances nitric oxide synthase-2 induction by IL-1β.
      FormWhite solid
      FormulationSupplied as a trifluoroacetate salt.
      Intert gas (Yes/No) Packaged under inert gas
      CAS number180977-44-0
      Chemical formulaC₂7H₃3N₃O₃S
      Structure formulaStructure formula
      Purity≥90% by HPLC
      SolubilityDMSO (5 mg/ml). Degas DMSO just prior to reconstitution.
      Storage -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Unstable in solution; reconstitute just prior to use.
      Toxicity Standard Handling
      ReferencesQian, Y., et al. 1998. Bioorg. Med. Chem. 6, 293.
      Finder, J.D., et al. 1997. J. Biol. Chem. 272, 13484.
      Miquel, K., et al. 1997. Cancer Res. 57, 1846.
      Vogt, A., et al. 1997. J. Biol. Chem. 272, 27224.
      McGuire, T., et al. 1996. J. Biol. Chem. 271, 27402.
      Vogt, A., et al. 1996. Oncogene 13, 1991.
      Citation
    • Niels W.C.J. van de Donk, et al. (2005) Geranylgeranylated proteins are involved in the regulation of myeloma cell growth. Clinical Cancer Research 11, 429-439.
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      Categories

      Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Other Inhibitors of Biological Interest > Farnesyltransferase (FTase), Geranylgeranyltransferase (GGTase), & Methyltransferase Inhibitors