For research use only
|Description||GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors.|
|IC50 & Target|
IC50: 9.5 nM (GGTase I), 53 μM (FTase)
|In Vitro||GGTI-2418 inhibits GGTase I and FTase activities with IC50s
of 9.5±2.0 nM and 53±11 μM, respectively, a 5,600-fold selectivity
toward inhibition of GGTase I versus FTase. GGTI-2418 demonstrates
competitive inhibition of GGTase I against the H-Ras-CVLL protein with a
Ki of 4.4±1.6 nM.|
GGTi-2418 (10-15 μM; 16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3.
|In solvent||-80°C||6 months|
. Kazi A, et al. Blockade of protein geranylgeranylation inhibits Cdk2-dependent p27Kip1 phosphorylation on Thr187 and accumulates p27Kip1 in the nucleus: implications for breast cancer therapy. Mol Cell Biol. 2009 Apr;29(8):2254-63.
. Kuchay S, et al. PTEN counteracts FBXL2 to promote IP3R3- and Ca2+-mediated apoptosis limiting tumour growth. Nature. 2017 Jun 22;546(7659):554-558.