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

GGTI-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.

GGTI-286 - CAS 171744-11-9 - Calbiochem : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: N-4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(L)-leucine methyl ester, TFA

Primary Target: Geranylgeranyltransferase (GGTase)
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345878
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Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
171744-11-9C₂₃H₃₁N₃O₃S

Prix & Disponibilité

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345878-250UG
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      		 Ampoule plast. 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 ImageStructure formula Image
      Quality LevelMQ100
      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
      Global Trade Item Number
      Référence GTIN
      345878-250UG 04055977214505

      Documentation

      GGTI-286 - CAS 171744-11-9 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      GGTI-286 - CAS 171744-11-9 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      345878

      Références bibliographiques

      Aperçu de la référence bibliographique
      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

      Titre
    • 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.
      		•
      Fiche technique

      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 formulaStructure 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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      Catégories

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