A cell-permeable triazolo-farnesylthiopropanoate compound that acts as a potent, reversible, and isoprenyl mimetic competitive inhibitor of isoprenylcysteine carboxyl methyltransferase activity (ICMT; IC50=800nM; Ki=400nM). 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 >100uM). Also shown to arrest the proliferation of PaTu-8902, a highly metastatic pancreatic cancer cells (IC50=8uM).
Formula:C26H31N3O2S
Molecular Weight:449.6
Solubility:DMSO (50mg/ml)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.