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| GGTI 2133 (trifluoroacetate salt) Basic information |
| GGTI 2133 (trifluoroacetate salt) Chemical Properties |
| Melting point | 103-118.5 °C | | storage temp. | -20°C |
| GGTI 2133 (trifluoroacetate salt) Usage And Synthesis |
| Description | GGTI 2133 is a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50 = 38 nM). It is 140-fold selective for GGTase I over farnesyltransferase (IC50 = 5,400 nM). In vitro, it inhibits geranylgeranylation of RAP1A (IC50 = 10 μM) without inhibiting farnesylation of H-Ras (IC50 = >30 μM). It also inhibits cell growth and decreases migration and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control values, respectively. GGTI 2133 (5 mg/kg per day, i.p.) prevents ovalbumin-induced eosinophil infiltration into airways in a mouse model of allergic bronchial asthma but does not prevent an increase in chemokines. It also blocks naloxone-induced contraction of ileum isolated from rats with morphine withdrawal syndrome and dose-dependently decreases withdrawal severity in vivo (ED50 = 0.076 mg/kg). | | Uses | GGTI-2133 has been used- To understand the role of geranylgeranyl transferase in the regulation of CXC chemokine production and neutrophil recruitment in the lung.
- To study the importance of geranylgeranylation in cell adhesion.
- To measure ligand-induced ADP-ribosylation factor 6 (Arf6) activation in breast cancer cells.
| | Biochem/physiol Actions | GGTase I mediates prenylation to induce the oncogenic functions of the Ras and Rho proteins. Thus, GGTase I inhibitors can be utilized as effective anticancer drugs. They are also useful in treating inflammation, atherosclerosis, multiple sclerosis and other diseases. |
| GGTI 2133 (trifluoroacetate salt) Preparation Products And Raw materials |
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