420351

ICMT Inhibitor II, FTPAT

The ICMT Inhibitor II, FTPAT controls the biological activity of ICMT.

• Synonym(s): ICMT Inhibitor II, FTPAT, ( E)-methyl-3-((5-(4-(2-((1,1ʹ-biphenyl]-4-yl)ethyl)-1H-1,2,3-triazol-1-yl)-3-methylpent-2-en-1-yl)thio)propanoate, (E)-methyl-3-((5-(4-(2-((1,1ʹ-biphenyl]-4-yl)ethyl)-1H-1,2,3-triazol-1-yl)-3-methylpent-2-en-1-yl)thio)propanoate
• Empirical Formula (Hill Notation): C₂₆H₃₁N₃O₂S
• CAS Number: 1350561-58-8
• Molecular Weight: 449.61
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: O=C(OC)CCSC/C=C(C)/CCN1N=NC(CCC2=CC=C(C3=CC=CC=C3)C=C2)=C1

Description

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).

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable