GGTI-286 是一种高效的细胞通透性 GGTase I 抑制剂，(IC50 为 2 μM。在 NIH3T3 细胞中，GGTI-286 对 Rap1A 香叶香叶基化的抑制作用高于 H-Ras 的法尼化作用 (IC50=2和 >30 μM)。GGTI-286 还能有效抑制 K-Ras4B 刺激，IC50 为 1 μM。
货号:ajcx37188
CAS:171744-11-9
分子式:C23H31N3O3S
分子量：429.58
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.