GGTI-286 is a selective inhibitor of geranylgeranyl transferase I (GGTase I) with an IC50 of 2 μM, demonstrating 25-fold increased potency compared to its methyl ester derivative. It effectively inhibits the geranylgeranylation of Rap1A while displaying a lower impact on the farnesylation of H-Ras, with IC50 values of 2 μM and >30 μM, respectively. Additionally, GGTI-286 shows strong inhibition of oncogenic K-Ras4B stimulation, with an IC50 of 1 μM, making it a valuable tool for research in cancer biology and signaling pathways.
GGTI-286 is a selective inhibitor of geranylgeranyl transferase I (GGTase I) with an IC50 of 2 μM, demonstrating 25-fold increased potency compared to its methyl ester derivative. It effectively inhibits the geranylgeranylation of Rap1A while displaying a lower impact on the farnesylation of H-Ras, with IC50 values of 2 μM and >30 μM, respectively. Additionally, GGTI-286 shows strong inhibition of oncogenic K-Ras4B stimulation, with an IC50 of 1 μM, making it a valuable tool for research in cancer biology and signaling pathways.
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