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345878 | GGTI-286 - CAS 171744-11-9 - Calbiochem

345878
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₃H₃₁N₃O₃S 171744-11-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      345878-250UG
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          Glass bottle 250 μg
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          Description
          OverviewA potent, cell-permeable, and selective inhibitor of GGTase I. This methyl ester derivative of GGTI-287 (Cat. No. 345880) is about 25-fold more potent (IC50 = 2 µM vs. 50 µM) than FTI-277 (Cat. No. 344555) in inhibiting the processing of the geranylgeranylated protein Rap1A. Selectively antagonizes oncogenic K-Ras4B (IC50 = 2 µM). GGTI-286 has also been shown to have a significant antiproliferative effect in human malignant glioma cells.
          Catalogue Number345878
          Brand Family Calbiochem®
          SynonymsN-4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(L)-leucine methyl ester, TFA
          References
          ReferencesBredel, M., et al. 1998. Neurosurgery 43, 124.
          Qian, Y., et al. 1998. Bioorg. Med. Chem. 6, 293.
          Lerner, E.C., et al. 1997. Oncogene 15, 1283.
          Lerner, E.C., et al. 1995. J. Biol. Chem. 270, 26770.
          Product Information
          CAS number171744-11-9
          ATP CompetitiveN
          FormGlassy solid
          FormulationSupplied as a trifluoroacetate salt.
          Hill FormulaC₂₃H₃₁N₃O₃S
          Chemical formulaC₂₃H₃₁N₃O₃S
          ReversibleN
          Structure formula Image
          Applications
          ApplicationGGTI-286, CAS 171744-11-9, is a cell-permeable, potent, and selective inhibitor of GGTase I. It is about 25-fold more potent (IC50 = 2 µM) than FTI-277 in inhibiting the processing of Rap1A protein.
          Biological Information
          Primary TargetGeranylgeranyltransferase (GGTase)
          Primary Target IC<sub>50</sub>2 µM against GGTase
          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 (-70°C). Stock solutions are stable for up to 1 week at -70°C.
          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
          345878

          References

          Reference overview
          Bredel, M., et al. 1998. Neurosurgery 43, 124.
          Qian, Y., et al. 1998. Bioorg. Med. Chem. 6, 293.
          Lerner, E.C., et al. 1997. Oncogene 15, 1283.
          Lerner, E.C., et al. 1995. J. Biol. Chem. 270, 26770.

          Citations

          Title
        • Karen E. Porter, et al. (2004) Simvastatin reduces human atrial myofibroblast proliferation independently of cholesterol lowering via inhibition of RhoA. Cardiovascular Research 61, 745-755.
        • 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.

          Revision31-March-2011 RFH
          SynonymsN-4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(L)-leucine methyl ester, TFA
          DescriptionA potent, cell-permeable, and selective GGTase-I inhibitor. This methyl ester derivative of GGTI-287 (Cat. No. 345880) is 25-fold more potent (IC50 = 2 µM versus 50 µM) than FTI-277 (Cat. No. 344555) inhibiting the processing of the geranylgeranylated protein Rap1A. Selectively antagonizes oncogenic K-Ras4B (IC50 = 2 µM). GGTI-286 has also been shown to have a significant antiproliferative effect in human malignant glioma cells.
          FormGlassy solid
          FormulationSupplied as a trifluoroacetate salt.
          Intert gas (Yes/No) Packaged under inert gas
          CAS number171744-11-9
          Chemical formulaC₂₃H₃₁N₃O₃S
          Structure formula
          Purity≥90% by HPLC
          SolubilityDMSO (10 mg/ml)
          Storage -20°C
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution aliquot and freeze (-70°C). Stock solutions are stable for up to 1 week at -70°C.
          Toxicity Standard Handling
          ReferencesBredel, M., et al. 1998. Neurosurgery 43, 124.
          Qian, Y., et al. 1998. Bioorg. Med. Chem. 6, 293.
          Lerner, E.C., et al. 1997. Oncogene 15, 1283.
          Lerner, E.C., et al. 1995. J. Biol. Chem. 270, 26770.
          Citation
        • Karen E. Porter, et al. (2004) Simvastatin reduces human atrial myofibroblast proliferation independently of cholesterol lowering via inhibition of RhoA. Cardiovascular Research 61, 745-755.
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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