420351
ICMT Inhibitor II, FTPAT
The ICMT Inhibitor II, FTPAT controls the biological activity of ICMT.
别名:
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
InChI key
LUXQNURJPSSXSC-RCCKNPSSSA-N
SMILES string
O=C(OC)CCSC/C=C(C)/CCN1N=NC(CCC2=CC=C(C3=CC=CC=C3)C=C2)=C1
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
Quality Level
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; 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
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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