Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 2 µM against GGTase

Primary TargetGeranylgeranyltransferase (GGTase)

Cell permeable: yes

General description

A potent, cell-permeable, and selective inhibitor of GGTase I. This methyl ester derivative of GGTI-287 (Cat. No. 345880) is about 25-fold more potent (IC₅₀ = 2 µM vs. 50 µM) than FTI-277 (Cat. No. 344555) in inhibiting the processing of the geranylgeranylated protein Rap1A. Selectively antagonizes oncogenic K-Ras4B (IC₅₀ = 2 µM). GGTI-286 has also been shown to have a significant antiproliferative effect in human malignant glioma cells.

A potent, cell-permeable, and selective GGTase-I inhibitor. This methyl ester derivative of GGTI-287 (Cat. No. 345880) is 25-fold more potent (IC₅₀ = 2 µM versus 50 µM) than FTI-277 (Cat. No. 344555) inhibiting the processing of the geranylgeranylated protein Rap1A. Selectively antagonizes oncogenic K-Ras4B (IC₅₀ = 2 µM). GGTI-286 has also been shown to have a significant antiproliferative effect in human malignant glioma cells.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Bredel, M., et al. 1998. Neurosurgery 43, 124.Qian, Y., et al. 1998. Bioorg. Med. Chem.6, 293.Lerner, E.C., et al. 1997. Oncogene 15, 1283.Lerner, E.C., et al. 1995. J. Biol. Chem. 270, 26770.

Packaging

Packaged under inert gas

250 µg in Plastic ampoule

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution aliquot and freeze (-70°C). Stock solutions are stable for up to 1 week at -70°C.

Warning

Toxicity: Standard Handling (A)