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; Ki = 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).
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Bergman, J.A., et al. 2012. ACS Med. Chem. Lett.3, 15.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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