WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406424
Description: 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.
MedKoo Cat#: 406424
Chemical Formula: C24H28N4O3
Exact Mass: 420.21614
Molecular Weight: 420.50412
Elemental Analysis: C, 68.55; H, 6.71; N, 13.32; O, 11.41
Synonym: GGTI2154; GGTI 2154; GGTI-2154.
IUPAC/Chemical Name: L-Leucine, N-[[5-[(1H-imidazol-4-ylmethyl)amino]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]-
InChi Key: GAJLKAVQYXFCRU-QFIPXVFZSA-N
InChi Code: InChI=1S/C24H28N4O3/c1-15(2)10-22(24(30)31)28-23(29)20-9-8-17(26-13-18-12-25-14-27-18)11-21(20)19-7-5-4-6-16(19)3/h4-9,11-12,14-15,22,26H,10,13H2,1-3H3,(H,25,27)(H,28,29)(H,30,31)/t22-/m0/s1
SMILES Code: CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CNC=N2)C=C1C3=CC=CC=C3C)=O
1: Sun J, Ohkanda J, Coppola D, Yin H, Kothare M, Busciglio B, Hamilton AD, Sebti SM. Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice. Cancer Res. 2003 Dec 15;63(24):8922-9. PubMed PMID: 14695209.