An indole-based

Cysmethynil – 10 mg

Brand:
Cayman
CAS:
851636-83-4
Storage:
-20
UN-No:
Non-Hazardous - /

Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. Isoprenylcysteine carboxyl methyltransferase (Icmt) catalyzes the methylation of C-terminal prenylcysteine residues, the last step in this process. Cysmethynil is an indole-based, time-dependent inhibitor of Icmt (IC50 = adenosylmethionine (Ki = 0.14 µM for the final complex).{23512} It does not inhibit other enzymes in the prenylation pathway (farensyltransferase, geranylgeranyltransferase type I, and Rce1) at concentrations up to 50 µM, or related methyltransferases.{23511} Treatment of cancer cells results in a dose-dependent decrease in Ras carboxylmethylation, mislocalization of Ras, and impaired signaling through Ras pathways.{23511} Treatment of PC3 prostate cancer cells with 25 µM cysmethynil resulted in decreased mTOR signaling, accumulation of cells in the G1 phase, and autophagy-mediated cell death.{23510}  

 

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Description

An indole-based, time-dependent inhibitor of Icmt (IC50 = i = 0.14 µM for the final complex); decreases mTOR signaling, accumulation of cells in the G1 phase, and autophagy-mediated cell death in PC3 prostate cancer cells

Formal name: 5-(3-methylphenyl)-1-octyl-1H-indole-3-acetamide

Synonyms:  Icmt Inhibitor

Molecular weight: 376.5

CAS: 851636-83-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Cancer|Autophagy||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy

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