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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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 593.66. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.25 mM||6.74 mL||33.69 mL||67.38 mL|
|1.25 mM||1.35 mL||6.74 mL||13.48 mL|
|2.5 mM||0.67 mL||3.37 mL||6.74 mL|
|12.5 mM||0.13 mL||0.67 mL||1.35 mL|
References are publications that support the biological activity of the product.
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
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
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
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Keywords: GGTI 298, GGTI 298 supplier, GGTI298, geranylgeranyltransferase, GGTase1, Protein, Prenyltransferases, Post-translational, Modifications, 2430, Tocris Bioscience
1 Citation for GGTI 298
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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