GGTI-286 |
| カタログ番号GC64216 |
強力で細胞透過性の GGTase I 阻害剤である GGTI-286 は、対応する FTI-276 のメチルエステルよりも 25 倍強力です (IC50 = 2 μM)。 GGTI-286 は、NIH3T3 細胞において、H-Ras のファルネシル化よりも Rap1A のゲラニルゲラニル化を選択的に阻害します (それぞれ、IC50 = 2 および >30 μM)。 GGTI-286 はまた、発癌性 K-Ras4B 刺激を 1 μM の IC50 で強力に阻害します。
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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