GGTI-286 hydrochloride |
| Katalog-Nr.GC64784 |
GGTI-286-Hydrochlorid, ein potenter GGTase-I-Inhibitor, ist 25-mal potenter (IC50 = 2 μM) als der entsprechende Methylester von FTI-276. GGTI-286-Hydrochlorid hemmt selektiv die Geranylgeranylierung von Rap1A gegenÜber der Farnesylierung von H-Ras in NIH3T3-Zellen (IC50s = 2 bzw. > 30 μM). GGTI-286-Hydrochlorid hemmt auch stark die onkogene K-Ras4B-Stimulation mit einem IC50 von 1 μM.
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Cas No.: 181141-66-2
Sample solution is provided at 25 µL, 10mM.
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GGTI-286 hydrochloride, a potent GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276 . GGTI-286 hydrochloride selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s =2 and >30 μM, respectively). GGTI-286 hydrochloride also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM[1][2].
[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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