GGTI 298

Cat. No. 2430

GGTI 298 C27H33N3O3S.CF3CO2H [1217457-86-7]

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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:
593.66
Formula:
C27H33N3O3S.CF3CO2H
Solubility:
Soluble to 25 mM in DMSO
Purity:
>95 %
Storage:
Store at -20°C
CAS No:
1217457-86-7

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Porcu et al (2010) A yeast-based genomic strategy highlights the cell protein networks altered by FTase inhibitor peptidomimetics. Mol.Cancer 9 197. PMID: 20653956.

Kusama et al (2003) Selective inhibition of cancer cell invasion by a geranylgeranyltransferase inhibitor. Clin.Exp.Meta. 20 561.

Miquel et al (1997) GGTI-298 induces G0-G1 block and apoptosis whereas FTI-227 causes G2-M enrichment in A549 cells. Cancer Res. 57 1846. PMID: 9157972.

McGuire et al (1996) Platelet-derived growth factor receptor tyrosine kinase phosphorylation requires protein geranylgeranylation but not farnesylation. J.Biol.Chem. 271 27402. PMID: 8910319.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for GGTI 298 include:

Domingue et al (2016) Chenodeoxycholic Acid Requires Activation of EGFR, EPAC and Ca2+ to Stimulate CFTR-dependent Cl-Secretion in Human Colonic T84 Cells. American Journal of Physiology - Cell Physiology. PMID: 27558159.

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Keywords: GGTI 298, supplier, GGTI298, geranylgeranyltransferase, GGTase1, Tocris Bioscience, Protein Prenyltransferase Inhibitor products

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