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 NumberAvailability Packaging Qty/Pack Price Quantity
      345883-1MG
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          Plastic ampoule 1 mg
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          345883-250UG
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              Glass bottle 250 μg
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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

              SDS

              Title

              Safety Data Sheet (SDS) 

              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