GGTI-286 |
| Catalog No.GC64216 |
Le GGTI-286, un inhibiteur de la GGTase I puissant et perméable aux cellules, est 25 fois plus puissant (IC50 = 2 μM) que l'ester méthylique correspondant du FTI-276. Le GGTI-286 inhibe sélectivement la géranylgéranylation de Rap1A par rapport À la farnésylation de H-Ras dans les cellules NIH3T3 (IC50 = 2 et > 30 μM, respectivement). Le GGTI-286 inhibe également puissamment la stimulation oncogène de K-Ras4B avec une IC50 de 1 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 171744-11-9
Sample solution is provided at 25 µL, 10mM.
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GGTI-286, a potent and cell-permeable GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276 . GGTI-286 selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s =2 and >30 μM, respectively). GGTI-286 also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM[1].
[1]. E C Lerner, et al. Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. J Biol Chem. 1995 Nov 10;270(45):26770-3. [2]. Naoyuki Nishiya, et al. A zebrafish chemical suppressor screening identifies small molecule inhibitors of the Wnt/β-catenin pathway. Chem Biol. 2014 Apr 24;21(4):530-540.
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