GGTI 298

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Description: Geranylgeranyltransferase I (GGTase I) inhibitor
Chemical Name: N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-(1-naphthalenyl)benzoyl]-L-leucine methyl ester trifluoroacetate salt
Purity: ≥95% (HPLC)
Citations (2)
Reviews (1)

Biological Activity for GGTI 298

GGTI 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.

Technical Data for GGTI 298

M. Wt 593.66
Formula C27H33N3O3S.CF3CO2H
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 1217457-86-7
PubChem ID 16078971
Smiles SC[C@H](N)CNC1=CC=C(C(N[C@H]([C@@](OC)=O)CC(C)C)=O)C(C2=CC=CC3=C2C=CC=C3)=C1.FC(F)(C(O)=O)F

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.

Solubility Data for GGTI 298

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 14.84 25

Preparing Stock Solutions for GGTI 298

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for GGTI 298

Certificate of Analysis / Product Datasheet
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References for GGTI 298

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

If you know of a relevant reference for GGTI 298, please let us know.

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Keywords: GGTI 298, GGTI 298 supplier, GGTI298, geranylgeranyltransferase, GGTase1, Protein, Prenyltransferases, Post-translational, Modifications, 2430, Tocris Bioscience

2 Citations 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

Luttman et al (2021) ABL allosteric inhibitors synergize with statins to enhance apoptosis of metastatic lung cancer cells. ABL allosteric inhibitors synergize with statins to 37 109880 PMID: 34706244

Do you know of a great paper that uses GGTI 298 from Tocris? Please let us know.

Reviews for GGTI 298

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Geranylgeranyltransferase I (GGTase I) inhibitor.
By Anonymous on 03/26/2018
Assay Type: In Vitro
Species: Rat

Geranylgeranyltransferase I (GGTase I) inhibitor

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