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.
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.
| Chemical | |
|---|---|
| CAS Num | 251577-10-3 |
| Chemical Formula | C24H28N4O3 |
| Molecular Weight | 420.50412 |
| IUPAC Chemical Name | L-Leucine, N-[[5-[(1H-imidazol-4-ylmethyl)amino]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]- |
| Exact Mass | 420.21614 |
| Elemental Analysis | C, 68.55; H, 6.71; N, 13.32; O, 11.41 |
| Synonym | GGTI2154; GGTI 2154; GGTI-2154. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CNC=N2)C=C1C3=CC=CC=C3C)=O |
| Biological | |
| Targets and Effects | geranylgeranyltransferase I |
| Pathways | Apoptosis |
| Physical | |
| Appearance | white solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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