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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) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: Geranylgeranyltransferase (GGTase)
345878
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
171744-11-9C₂₃H₃₁N₃O₃S

Products

Catalogue NumberPackaging Qty/Pack
345878-250UGCN Plastic ampoule 250 μg
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
Catalogue Number GTIN
345878-250UGCN 04055977214505

Documentation

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

Title

Safety Data Sheet (SDS) 

GGTI-286 - CAS 171744-11-9 - Calbiochem 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 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.
    		•