171744-11-9

171744-11-9 structure

Name: GGTI-286
Chemical Name: Methyl N-[(5-{[(2R)-2-amino-3-sulfanylpropyl]amino}-2-biphenylyl)carbonyl]-L-leucinate
CAS Number: 171744-11-9
Molecular Formula: C₂₃H₃₁N₃O₃S
Molecular Weight: 429.58
Catalog: Signaling Pathways GPCR/G Protein Ras
Create Date: 2018-06-12 13:07:18
Modify Date: 2024-01-08 10:55:40
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 (HY-15873A). 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].

Name	Methyl N-[(5-{[(2R)-2-amino-3-sulfanylpropyl]amino}-2-biphenylyl)carbonyl]-L-leucinate
Synonyms	L-Leucine, N-[[5-[[(2R)-2-amino-3-mercaptopropyl]amino][1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester Methyl N-[(5-{[(2R)-2-amino-3-sulfanylpropyl]amino}-2-biphenylyl)carbonyl]-L-leucinate methyl N-[(5-{[(2R)-2-amino-3-sulfanylpropyl]amino}biphenyl-2-yl)carbonyl]-L-leucinate GGTI-286

Description	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 (HY-15873A). 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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> GPCR/G Protein >> Ras
Target	IC50: 2 μM (Geranylgeranylation of Rap1A) in NIH3T3 cells[1]
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.

Hazard Codes	Xi