GGTI-286 |CAS:171744-11-9 Probechem Biochemicals

Chemical Structure : GGTI-286

GGTI-286 (GGTI286)

Catalog No.: PC-62472Not For Human Use, Lab Use Only.

GGTI-286 is a CAAX peptidomimetic, potent, cell-permeable, and selective inhibitor of GGTase I with IC50 of 2 uM, 25-fold more potent than FTI-277.

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Biological Activity

GGTI-286 is a CAAX peptidomimetic, potent, cell-permeable, and selective inhibitor of GGTase I with IC50 of 2 uM, 25-fold more potent than FTI-277.
GGTI-286 inhibits processing of the geranylgeranylated protein Rap1A; inhibits oncogenic K-Ras4B stimulation with IC50 of 1 uM.
GGTI-286 reduces nuclear localization of β-catenin and transcription dependent on β-catenin/T cell factor in mammalian cells.
GGTI-286 has significant antiproliferative effect in human malignant glioma cells.

Physicochemical Properties

M.Wt	429.579
Formula	C23H31N3O3S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	L-Leucine, N-[[5-[(2-amino-3-mercaptopropyl)amino][1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester, (R)-

References

1. Lerner EC, et al. J Biol Chem. 1995 Nov 10;270(45):26770-3.

2. Nishiya N, et al. Chem Biol. 2014 Apr 24;21(4):530-40.

3. Lerner EC, et al. Oncogene. 1997 Sep;15(11):1283-8.

GGTI-286 (GGTI286)

Biological Activity

Physicochemical Properties

References

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