GGTI298 trifluoroacetate salt hydrate
| CAS No. | 1217457-86-7 | Cat. No. | BCP24853 |
| Name | GGTI298 trifluoroacetate salt hydrate | ||
| Synonyms | GGTI-298 TFA; GGTI-298 trifluoride salt;GGTI298 Trifluoroacetate ;GGT-I298 trifluoroacetate salt hydrate; | ||
| Formula | C29H34F3N3O5S | M. Wt | 593.66 |
| Description | GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.GGTI-298 is a potent geranylgeranyltransferase-I (GGTase-I) inhibitor with potential antitumor actrivity. GGTI-298 disrupts MAP kinase activation and G(1)-S transition in Ki-Ras-overexpressing transformed adrenocortical cells. GGTI-298 induces hypophosphorylation of retinoblastoma and partner switching of cyclin-dependent kinase inhibitors. A potential mechanism for GGTI-298 antitumor activity. GGTI-298 arrests human tumor cells in G0/G1 and induces p21(WAF1/CIP1/SDI1) in a p53-independent manner. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells. | ||
| Pathways | GPCR/G Protein | ||
| Targets | Ras/Rho | ||
Structure
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