GGTI-286 dihydrochloride

Modify Date: 2024-04-02 14:47:28

GGTI-286 dihydrochloride Structure
GGTI-286 dihydrochloride structure
Common Name GGTI-286 dihydrochloride
CAS Number 181141-66-2 Molecular Weight 466.037
Density N/A Boiling Point N/A
Molecular Formula C23H32ClN3O3S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GGTI-286 dihydrochloride


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

 Names

Name GGTI-286 dihydrochloride

 GGTI-286 dihydrochloride Biological Activity

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

 Chemical & Physical Properties

Molecular Formula C23H32ClN3O3S
Molecular Weight 466.037