Chemical Name: N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-(1-naphthalenyl)benzoyl]-L-leucine methyl ester trifluoroacetate salt
Biological ActivityGGTI 298 is a 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Platelet-derived growth factor receptor tyrosine kinase phosphorylation requires protein geranylgeranylation but not farnesylation.
McGuire et al.
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
A yeast-based genomic strategy highlights the cell protein networks altered by FTase inhibitor peptidomimetics.
Porcu et al.
Selective inhibition of cancer cell invasion by a geranylgeranyltransferase inhibitor.
Kusama et al.
Citation for GGTI 298
The citations listed below are publications that use Tocris products. Selected citations for GGTI 298 include:
1 Citation: Showing 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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Geranylgeranyltransferase I (GGTase I) inhibitor