251577-10-3
251577-10-3
Chemical Structure
GGTI-2154
- CAS No.: 251577-10-3
- Formula:C24H28N4O3
- Molecular Weight:420.50
IUPAC Name: (5-(((1H-imidazol-5-yl)methyl)amino)-2'-methyl-[1,1'-biphenyl]-2-carbonyl)-L-leucine
InChIKey: GAJLKAVQYXFCRU-QFIPXVFZSA-N
SMILES: CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CN=CN2)C=C1C3=CC=CC=C3C)=O
Biological Activity: GGTI-2154 is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 can be used for the research of cancer[1][2].
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GGTI-2154 | GGTI-2154 is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 can be used for the research of cancer. | |||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
