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

345883
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂7H₃3N₃O₃S 180977-44-0

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      345883-1MG
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          Plastic ampoule 1 mg
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          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
          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

          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