General description

A cell-permeable triazolo-farnesylthiopropanoate compound that acts as a potent, reversible, and isoprenyl mimetic competitive inhibitor of isoprenylcysteine carboxyl methyltransferase activity (ICMT; IC₅₀ = 800 nM; K_i = 400 nM). Shown to prevent K-Ras membrane localization in GFP-K-Ras transfected Jurkat T-cells. Exhibits selective toxicity towards wt-Icmt^+/+ mouse embryonic fibroblasts (MEFs) over Icmt^-/- MEFs (IC₅₀ = 33 and >100 µM). Also shown to arrest the proliferation of PaTu-8902, a highly metastatic pancreatic cancer cells (IC₅₀ = 8 µM).

Legal Information

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

Other Notes

Bergman, J.A., et al. 2012. ACS Med. Chem. Lett.3, 15.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)