Molecular structure of GGTI-2133, CAS Number: 1217480-14-2
GGTI-2133 (CAS 1217480-14-2)
See product citations (2)
Alternate Names:
N-[[4-(Imidazol-4-yl)methylamino]-2-(1-naphthyl)benzoyl]leucine trifluoroacetate salt
Application:
GGTI-2133 is potent and selective GGTase I inhibitor
CAS Number:
1217480-14-2
Molecular Weight:
570.56
Molecular Formula:
C27H28N4O3•C2HF3O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Product Citations
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
GGTI-2133 is a potent, selective, non-thiol peptidomimetic inhibitor of geranylgeranyltransferase I (GGTase I), displaying 140-fold greater selectivity over farnesyltransferase with an IC50 of 38 nM. It is cell-permeable and may act to specifically inhibit the enzyme′s activity, including the geranylgeranylation of RAP1A, with an IC50 of 10 µM, while not significantly affecting H-Ras farnesylation. The compound influences cell behavior, notably inhibiting cell growth and reducing cell migration and invasion in specific cell lines. It has been studied for its effects in various models, including a demonstration of its impact on cell processes and behaviors.
GGTI-2133 (CAS 1217480-14-2) References
- Mevalonate sensitizes the nociceptive transmission in the mouse spinal cord. | Ohsawa, M., et al. 2008. Pain. 134: 285-292. PMID: 17764839
- Inhibition of geranylgeranyltransferase inhibits bronchial smooth muscle hyperresponsiveness in mice. | Chiba, Y., et al. 2009. Am J Physiol Lung Cell Mol Physiol. 297: L984-91. PMID: 19717551
- GGTI-2133, an inhibitor of geranylgeranyltransferase, inhibits infiltration of inflammatory cells into airways in mouse experimental asthma. | Chiba, Y., et al. 2009. Int J Immunopathol Pharmacol. 22: 929-35. PMID: 20074456
- R-Ras interacts with filamin a to maintain endothelial barrier function. | Griffiths, GS., et al. 2011. J Cell Physiol. 226: 2287-96. PMID: 21660952
- Geranylgeranyl transferase regulates CXC chemokine formation in alveolar macrophages and neutrophil recruitment in septic lung injury. | Hasan, Z., et al. 2013. Am J Physiol Lung Cell Mol Physiol. 304: L221-9. PMID: 23241528
- Simvastatin and GGTI-2133, a geranylgeranyl transferase inhibitor, increase erythrocyte deformability but reduce low O(2) tension-induced ATP release. | Clapp, KM., et al. 2013. Am J Physiol Heart Circ Physiol. 304: H660-6. PMID: 23335799
- Geranylgeranyl transferase regulates streptococcal M1 protein-induced CXC chemokine formation and neutrophil recruitment in the lung. | Zhang, S., et al. 2013. Shock. 39: 293-8. PMID: 23364431
- Pharmacological modulation of geranylgeranyltransferase and farnesyltransferase attenuates opioid withdrawal in vivo and in vitro. | Rehni, AK. and Singh, TG. 2013. Neuropharmacology. 71: 19-26. PMID: 23415632
- Inhibition of geranylgeranyltransferase attenuates neutrophil accumulation and tissue injury in severe acute pancreatitis. | Merza, M., et al. 2013. J Leukoc Biol. 94: 493-502. PMID: 23744643
- Simvastatin induces a central hypotensive effect via Ras-mediated signalling to cause eNOS up-regulation. | Cheng, WH., et al. 2013. Br J Pharmacol. 170: 847-58. PMID: 23889671
- Involvement of protein isoprenylation in neuropathic pain induced by sciatic nerve injury in mice. | Ohsawa, M., et al. 2014. Neurosci Lett. 564: 27-31. PMID: 24486886
- Statin-mediated inhibition of cholesterol synthesis induces cytoprotective autophagy in human leukemic cells. | Vilimanovich, U., et al. 2015. Eur J Pharmacol. 765: 415-28. PMID: 26358205
- Inhibition of the mevalonate pathway augments the activity of pitavastatin against ovarian cancer cells. | Abdullah, MI., et al. 2017. Sci Rep. 7: 8090. PMID: 28808351
Inhibitor of:
Enzyme, FACE-1, GGTase, GGTase-Iα, GGTase-Iβ, R-ras3, Rab 1B, Rab 35, RASL11A, and RGL4.Activator of:
GGTase-Iα, ICMT, PIG-Q, Rab 20, RCE1, and ZIP-kinase.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GGTI-2133, 1 mg | sc-221668 | 1 mg | $215.00 | |||
GGTI-2133, 5 mg | sc-221668A | 5 mg | $620.00 |