GGTI 298

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Cat.No. 2430 - GGTI 298 | C27H33N3O3S.CF3CO2H | CAS No. 1217457-86-7
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)
Datasheet
Citations (1)
Literature

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
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 1217457-86-7
PubChem ID 16078971
InChI Key WALKWJPZELDSKT-UFABNHQSSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

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 solvent 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
1 mM 1.68 mL 8.42 mL 16.84 mL
5 mM 0.34 mL 1.68 mL 3.37 mL
10 mM 0.17 mL 0.84 mL 1.68 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:


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Keywords: GGTI298 geranylgeranyltransferase GGTase1 Protein Prenyltransferases

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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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis

Pathways for GGTI 298

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