GGTI-286 |
| Catalog No.GC64216 |
강력하고 세포 투과성인 GGTase I 억제제인 GGTI-286은 FTI-276의 상응하는 메틸 에스테르보다 25배 더 강력합니다(IC50=2μM). GGTI-286은 NIH3T3 세포에서 H-Ras의 파르네실화보다 Rap1A의 게라닐게라닐화를 선택적으로 억제합니다(각각 IC50 =2 및 >30 μM). GGTI-286은 또한 1μM의 IC50으로 발암성 K-Ras4B 자극을 강력하게 억제합니다.
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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