420350
ICMT Inhibitor
2-(5-(3-Methylphenyl)-1-octyl-1H-indol-3-yl)acetamide, 2-(1-Octyl-5-m-tolyl-1H-indol-3-yl) acetamide, Cysmethynil, Cysmethynil, Isoprenylcysteine Carboxyl Methyltransferase Inhibitor
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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Telefon: +49 6151 72-0
Fax: +49 6151 72 2000
24 Mai 2013
wird geladen
A cell-permeable indole acetamide that acts as a substrate-competitive and AdoMet-noncompetitive Icmt (isoprenylcysteine carboxyl methyltransferase) inhibitor (Ki = 0.02 µM; IC50 = 0.29 µM; Substrate = S-farnesyl-L-cysteine), exhibiting no activity against FTase, gernaylgeranyltransferase type I, CaaX protease Rce1, AdoMet-dependent DNA methyltransferase, SssI DNA methyltransferase, or PCMT1 protein methyltransferase. Cysmethynil (25 µM) induces G1 cell cycle-arrest and autophagy-mediated, but not apoptotic, cell death in prostate cancer PC3 cells with concomitant PI 3-K/Akt and mTOR signaling blockage, consistent with inhibition of Icmt-mediated activation of Ras and Rheb GTPases. Murine PC3 xenograft studies reveal limited in vivo efficacy.
| Produktinformationen | |||
|---|---|---|---|
| Form | Pale yellow semi-solid | ||
| Molare Masse | 376.5 | ||
| Protect from Light | Ja | ||
| Packaged under inert gas | Ja | ||
| Purity | ≥95% by HPLC | ||
| Löslichkeit in Wasser | DMSO | ||
| Chemische Formel | C25H32N20 | ||
| Lager- und Versandinformationen | |||
|---|---|---|---|
| Lagerkategorie | -20°C | ||
| Ship |
Shipped with Blue Ice or with Dry Ice
Regulatory Review |
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