For research use only. Not for therapeutic Use.
GGTI-2154 hydrochloride is a potent and selective inhibitor geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 hydrochloride shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 hydrochloride can be used for the research of cancer[1][2].
GGTI-2154 inhibits the transfer of geranylgeranyl from [3H]GGPP to H-Ras CVLL, with an IC50 of 21 nM[1].
GGTI-2154 (100 mg/kg/day; s.c. for 14 days) induces breast tumor regression in MMTV-ν-Ha-Ras transgenic mice[2].
GGTI-2154 (50 mg/kg/day; i.p. for 50 day) inhibits A-549 tumor growth in nude mice by 60%[1].
| Catalog Number | I045066 |
| CAS Number | 478908-50-8 |
| Synonyms | (2S)-2-[[4-(1H-imidazol-5-ylmethylamino)-2-(2-methylphenyl)benzoyl]amino]-4-methylpentanoic acid;hydrochloride |
| Molecular Formula | C24H29ClN4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H28N4O3.ClH/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);1H/t22-;/m0./s1 |
| InChIKey | JQRKKNPKMYXQRS-FTBISJDPSA-N |
| SMILES | CC1=CC=CC=C1C2=C(C=CC(=C2)NCC3=CN=CN3)C(=O)NC(CC(C)C)C(=O)O.Cl |
| Reference | [1]. Sun J, et, al. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine. Cancer Res. 1999 Oct 1;59(19):4919-26. [2]. Sun J, et, al. 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. |
