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GGTI-286

Names

[ CAS No. ]:
171744-11-9

[ Name ]:
GGTI-286

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
626.9±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C23H31N3O3S

[ Molecular Weight ]:
429.58

[ Flash Point ]:
332.9±31.5 °C

[ Exact Mass ]:
429.208618

[ LogP ]:
3.76

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.588

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds