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.
Biochem/physiol Actions
Cell permeable: yes
Product does not compete with ATP.
Reversible: no
Target IC50: 75 nM against Ftase
Other Notes
Manne, V., et al. 1995. Drug Development Res.34, 121.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,desiccated (hygroscopic) |
| color | white |
| solubility | water: ≥10 mg/mL |
| shipped in | ambient |
| storage temp. | −20°C |
