GGTI-286 hydrochloride

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GGTI-286 hydrochloride 

GGTI-286 hydrochloride 是一种高效的 GGTase I 抑制剂，IC50 为 2 μM。在 NIH3T3 细胞中，GGTI-286 hydrochloride 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 hydrochloride 还能有效抑制 K-Ras4B，IC50 为 1 μM。

GGTI-286 hydrochloride

GGTI-286 hydrochloride Chemical Structure

CAS No. : 181141-66-2

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生物活性

GGTI-286 hydrochloride, a potent GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276 (HY-15873A). 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].

IC50 & Target

IC50: 2 μM (Geranylgeranylation of Rap1A) in NIH3T3 cells[1]
分子量

466.04

Formula

C23H32ClN3O3S
CAS 号

181141-66-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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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