Biochem/physiol Actions

Cell permeable: no

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 500 pM against FTase in vitro

Primary TargetFTase in vitro

General description

A highly potent and selective CAAX peptidomimetic of the carboxyl terminal of Ras proteins that inhibits farnesyl transferase (FTase) in vitro (IC₅₀ = 500 pM). Inhibits geranylgeranyltransferase I (GGTase I) at much higher concentration (IC₅₀ = 50 nM). Has been shown to selectively block the growth of a human lung carcinoma expressing oncogenic K-Ras in nude mice. Also inhibits oncogenic signaling and tumor growth of NIH 3T3 cells transformed with the Ras oncogene at 20 µM.

Legal Information

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

Other Notes

Lantry, L.E., et al. 2000. Carcinogenesis21, 113.Lerner, E.C., et al. 1995. J. Biol. Chem. 270, 26802.Sun, J., et al. 1995. Cancer Res. 55, 4243.

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)