Biochem/physiol Actions

Target IC₅₀: 75 nM against Ftase

Reversible: no

Product does not compete with ATP.

Cell permeable: yes

General description

A cell permeable potent and selective inhibitor of farnesyltransferase (FTase; IC₅₀ = 75 nM). Also inhibits Ras farnesylation in whole cells by ~90% at 25-250 µM. Resistant to cleavage by phosphorylation.Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

A highly selective and potent inhibitor of Ras farnesyltransferase (IC₅₀ = 75 nM). Inhibits geranylgeranyltransferase I (IC₅₀ = 24 µM) and II (IC₅₀ = 24 µM) at much higher concentrations. Also inhibits Ras farnesylation in whole cells by ~90% at 10-100 µg/ml (25-250 µM). Resistant to cleavage by phosphorylation.

Legal Information

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

Other Notes

Manne, V., et al. 1995. Drug Development Res.34, 121.

Packaging

1 mg in Plastic ampoule

Warning

Toxicity: Standard Handling (A)