Molecular structure of GGTI-2147
GGTI-2147
Application:
GGTI-2147 is a non-thiol peptidomimetic that inhibits GGTase I and blocks geranyl-geranylation of Rap1A
Purity:
≥95%
Molecular Weight:
470.6
Molecular Formula:
C28H30N4O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
GGTI-2147 is a cell-permeable non-thiol peptidomimetic that acts as a strong and selective inhibitor of GGTase I. Blocks the geranyl-geranylation of Rap1A with an IC50 value that is over 60-fold lower than that required to disrupt the farnesylation of H-Ras. GGTI-2147 is an inhibitor of FACE-1.
GGTI-2147 References
- Inhibition of glucose- and calcium-induced insulin secretion from betaTC3 cells by novel inhibitors of protein isoprenylation. | Amin, R., et al. 2002. J Pharmacol Exp Ther. 303: 82-8. PMID: 12235236
- Synergistic cytotoxic effects in myeloid leukemia cells upon cotreatment with farnesyltransferase and geranylgeranyl transferase-I inhibitors. | Morgan, MA., et al. 2003. Leukemia. 17: 1508-20. PMID: 12886237
- Novel roles for the rho subfamily of GTP-binding proteins in succinate-induced insulin secretion from betaTC3 cells: further evidence in support of the succinate mechanism of insulin release. | Kowluru, A., et al. 2003. Endocr Res. 29: 363-76. PMID: 14535637
- Depletion of substrates for protein prenylation increases apoptosis in human periovulatory granulosa cells. | Rung, E., et al. 2006. Mol Reprod Dev. 73: 1277-83. PMID: 16868926
- Dominant-negative alpha-subunit of farnesyl- and geranyltransferase inhibits glucose-stimulated, but not KCl-stimulated, insulin secretion in INS 832/13 cells. | Veluthakal, R., et al. 2007. Diabetes. 56: 204-10. PMID: 17192483
- Down-regulation of RhoA is involved in the cytotoxic action of lipophilic statins in HepG2 cells. | Maeda, A., et al. 2010. Atherosclerosis. 208: 112-8. PMID: 19683239
- Characterization of the in vitro activity of AZD3409, a novel prenyl transferase inhibitor. | Appels, NM., et al. 2011. Cancer Chemother Pharmacol. 67: 137-45. PMID: 20229082
- Phagocyte-like NADPH oxidase promotes cytokine-induced mitochondrial dysfunction in pancreatic β-cells: evidence for regulation by Rac1. | Subasinghe, W., et al. 2011. Am J Physiol Regul Integr Comp Physiol. 300: R12-20. PMID: 20943855
- Phagocyte-like NADPH oxidase generates ROS in INS 832/13 cells and rat islets: role of protein prenylation. | Syed, I., et al. 2011. Am J Physiol Regul Integr Comp Physiol. 300: R756-62. PMID: 21228337
- RhoA regulates invasion of glioma cells via the c-Jun NH2-terminal kinase pathway under hypoxia. | Tong, JJ., et al. 2012. Oncol Lett. 4: 495-500. PMID: 23741249
- Inhibiting geranylgeranyltransferase I activity decreases spine density in central nervous system. | Yuan, M., et al. 2015. Hippocampus. 25: 373-84. PMID: 25330763
- Astrocyte GGTI-mediated Rac1 prenylation upregulates NF-κB expression and promotes neuronal apoptosis following hypoxia/ischemia. | Gao, S., et al. 2016. Neuropharmacology. 103: 44-56. PMID: 26690896
- Metabolic Stress Induces Caspase-3 Mediated Degradation and Inactivation of Farnesyl and Geranylgeranyl Transferase Activities in Pancreatic β-Cells. | Veluthakal, R., et al. 2016. Cell Physiol Biochem. 39: 2110-2120. PMID: 27802439
Inhibitor of:
Enzyme, FACE-1, and GGTase.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GGTI-2147, 250 µg | sc-221669 | 250 µg | $269.00 |