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GGTI-2154 GGTI-2154 is a geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2154 results not only in halting the growth of aggressive breast tumors but actually in inducing the regression (54 +/- 3%) of all 19 tumors analyzed. The farnesyltransferase (FTase) inhibitor FTI-2148 induced an average of 87 +/- 3% regression in the 13 tumors analyzed. GGTase I, but not FTase, is inhibited in breast tumors after treatment with GGTI-2154, whereas in tumors from mice treated with FTI-2148, only FTase is inhibited. The processing of the geranylgeranylated proteins RhoA, Rap1, and R-Ras, but not the farnesylated proteins H-Ras and HDJ-2, is inhibited in tumors obtained from mice treated with GGTI-2154. GGTI-2154 and FTI-2148 suppress constitutively activated phospho-Erk1/2 and phospho-Akt, induce apoptosis, and induce differentiation toward ductolobular breast epithelium. Synonyms: GGTI-2154; GGTI 2154; GGTI2154. Grade: 98%. CAS No. 251577-10-3. Molecular formula: C24H28N4O3. Mole weight: 420.51. BOC Sciences 8
GGTI-2154 hydrochloride GGTI-2154 hydrochloride is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. It shows more than 200-fold selectivity for GGTase I over FTase (IC50 = 5600 nM). Grade: 98%. CAS No. 478908-50-8. Molecular formula: C24H29ClN4O3. Mole weight: 456.97. BOC Sciences 8

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