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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: MSDS (material safety data sheet) o SDS, certificato d’analisi (CoA) e certificato di qualità (CoQ), dossier, brochure e altri documenti disponibili.

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

Primary Target: Geranylgeranyltransferase (GGTase)
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Replacement Information

Tabella delle specifiche principali

CAS #Empirical Formula
171744-11-9C₂₃H₃₁N₃O₃S

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Numero di catalogo DisponibilitàConfezionamento Qtà/conf Prezzo Quantità
345878-250UG
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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
      Numero di catalogo GTIN
      345878-250UG 04055977214505

      Documentation

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

      Titolo

      Scheda di sicurezza (MSDS) 

      GGTI-286 - CAS 171744-11-9 - Calbiochem Certificati d'Analisi

      TitoloNumero di lotto
      345878

      Riferimenti bibliografici

      Panoramica delle referenze
      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.

      Citazioni

      Titolo
    • 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.
      		•
      Scheda tecnica

      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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      Categorie

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