Catalog Number: 2430
Chemical Name: N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-(1-naphthalenyl)benzoyl]-L-leucine methyl ester trifluoroacetate salt
Biological Activity
CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor. Strongly inhibits the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras (IC50 values are 3 and > 10 μM respectively). Causes G0-G1 cell cycle block and apoptosis in A549 cells and inhibits cell invasion and migration in COLO 320CM cells.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 25 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Platelet-derived growth factor receptor tyrosine kinase phosphorylation requires protein geranylgeranylation but not farnesylation.
    McGuire et al.
    J.Biol.Chem., 1996;271:27402
  2. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-227 causes G2-M enrichment in A549 cells.
    Miquel et al.
    Cancer Res., 1997;57:1846
  3. A yeast-based genomic strategy highlights the cell protein networks altered by FTase inhibitor peptidomimetics.
    Porcu et al.
    Mol.Cancer, 2010;9:197
  4. Selective inhibition of cancer cell invasion by a geranylgeranyltransferase inhibitor.
    Kusama et al.
    Clin.Exp.Meta., 2003;20:561

The citations listed below are publications that use Tocris products. Selected citations for GGTI 298 include:

1 Citations: Showing 1 - 1

  1. Chenodeoxycholic Acid Requires Activation of EGFR, EPAC and Ca2+ to Stimulate CFTR-dependent Cl-Secretion in Human Colonic T84 Cells.
    Authors: Domingue Et al.
    American Journal of Physiology - Cell Physiology 2016;

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