Cat. No. 2430
Chemical Name: N-[4-[2(R)-Amino-3-mercaptopropyl]a
Biological ActivityCAAZ 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.
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 Datasheet
References are publications that support the products' biological activity.
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 GGTI 298 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.
Do you know of a great paper that uses GGTI 298 from Tocris? If so please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: GGTI 298, supplier, GGTI298, geranylgeranyltransferase, GGTase1, Tocris Bioscience, Protein Prenyltransferase Inhibitor products
Find multiple products by catalog number
New Products in this Area
Highly potent and SAM-competitive EZH2 inhibitorGSK 591 dihydrochloride
Potent and selective PRMT5 inhibitorTP 064
Potent and selective PRMT 4 inhibitor
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.