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GGTI-286 (TFA)
Products Details
Product Description
– 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].
Web ID
– HY-115489A
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C25H32F3N3O5S
References
– [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.
Molecular Weight
– 543.60
SMILES
– 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
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Ras
Pathway
– GPCR/G Protein
Product type
– Reference compound
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