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GGTI-2154

Chemical Structure : GGTI-2154

CAS No.: 251577-10-3

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GGTI-2154 (GGTI 2154)

Catalog No.: PC-22627Not For Human Use, Lab Use Only.

GGTI-2154 is a potent, selective inhibitor geranylgeranyltransferase I (GGTase I) with IC50 f 21 nM, >250-fold selective over FTase.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GGTI-2154 is a potent, selective inhibitor geranylgeranyltransferase I (GGTase I) with IC50 f 21 nM, >250-fold selective over FTase.
GGTI-2154 inhibits the processing of the geranylgeranylated proteins RhoA, Rap1, and R-Ras, but not the farnesylated proteins H-Ras and HDJ-2, in tumors obtained from mice.
GGTI-2154 suppresses constitutively activated phospho-Erk1/2 and phospho-Akt, induce apoptosis, and induce differentiation toward ductolobular breast epithelium.

Physicochemical Properties

M.Wt 420.51
Formula C24H28N4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

L-Leucine, N-[[5-[(1H-imidazol-5-ylmethyl)amino]-2′-methyl[1,1′-biphenyl]-2-yl]carbonyl]-

References

1. Sun J, et al. Cancer Res. 1999 Oct 1;59(19):4919-26.

2. Sun J, et al. Cancer Res. 2003 Dec 15;63(24):8922-9.

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