GGTI-286 TFA 

GGTI-286 TFA, a potent and cell-permeable GGTase I inhibitor, is 25-fold more potent (IC₅₀=2 μM) than the corresponding methyl ester of FTI-276 (HY-15873A). GGTI-286 TFA selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC₅₀s=2 and >30 μM, respectively). GGTI-286 TFA also potently inhibits oncogenic K-Ras4B stimulation with an IC₅₀ of 1 μM^[1][2].

GGTI-286 (10 μM; 2 and 4 h; CHO cells) TFA reduces nuclear localization of β-catenin and transcription dependent on β-catenin/T cell factor in mammalian cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

543.60

C₂₅H₃₂F₃N₃O₅S

Solid

White to off-white

CC(C)C[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2)=O.OC(C(F)(F)F)=O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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.  [Content Brief]

  [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.  [Content Brief]