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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C26H31N3O2S
CAS Number:
1350561-58-8
Molecular Weight:
449.61
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light

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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

100

Related Categories

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)

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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