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Chemical Structure : Cysmethynil
Catalog No.: PC-70250Not For Human Use, Lab Use Only.
A selective small-molecule inhibitor of tisoprenylcysteine carboxyl methyltransferase (Icmt) with IC50 <200 nM, does not inhibit other enzymes (farensyltransferase, geranylgeranyltransferase type I, and Rce1) at concentrations up to 50 uM.
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A selective small-molecule inhibitor of tisoprenylcysteine carboxyl methyltransferase (Icmt) with IC50 <200 nM, does not inhibit other enzymes (farensyltransferase, geranylgeranyltransferase type I, and Rce1) at concentrations up to 50 uM; acts as a competitive inhibitor with respect to the isoprenylated cysteine substrate and a noncompetitive inhibitor with respect to S-adenosylmethionine (Ki=0.14 uM); causes decrease in Ras carboxylmethylation, mislocalization of Ras, and impaired signaling through Ras pathways, reduces mTOR signaling and results in both an accumulation of cells in the G(1) phase and cell death in PC3 cells.
| M.Wt | 376.5 | |
| Formula | C25H32N2O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Winter-Vann AM, et al. Proc Natl Acad Sci U S A. 2005 Mar 22;102(12):4336-41.
2. Baron RA, et al. Biochemistry. 2007 Jan 16;46(2):554-60.
3. Wang M, et al. J Biol Chem. 2008 Jul 4;283(27):18678-84.
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