GGTase Inhibitor

BAY-593 is an orally active GGTase-I inhibitor. BAY-593 can block YAP1/TAZ signaling in animals and has antitumor activity.

GGTI-2154 hydrochloride is a potent and selective inhibitor geranylgeranyltransferase I (GGTase I), with an IC₅₀ of 21 nM. GGTI-2154 hydrochloride shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 hydrochloride can be used for the research of cancer.

GGTI-2133, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC₅₀ of 38 nM. GGTI-2133 shows 140-fold selectivity over farnesyltransferase (FTase) (IC₅₀ of 5.4 μM). GGTI-2133 inhibits the geranylation of Rap-1A with an IC₅₀ of 10 μM. GGTI-2133 can be used for the study of eosinophilic airway inflammation such as asthma.

(7S)-BAY-593 is the S-enantiomer of BAY-593 (HY-161573). BAY-593 is an orally active GGTase-I inhibitor. BAY-593 can block YAP1/TAZ signaling in animals and has antitumor activity.

GGTI-2166 is a geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2166 blocks geranylgeranylation modification of target proteins. GGTI-2166 inhibits RANKL- or TNF-α-induced pre-osteoclast formation and TRAP activity. GGTI-2166 is applicable to research on osteoclast differentiation.

GGTI-2133 TFA, a peptidomimetic, is a selective geranylgeranyltransferase I (GGTase-I) inhibitor with an IC₅₀ of 38 nM. GGTI-2133 TFA shows 140-fold selectivity over farnesyltransferase (FTase) (IC₅₀ of 5.4 μM). GGTI-2133 TFA inhibits the geranylation of Rap-1A with an IC₅₀ of 10 μM. GGTI-2133 TFA can be used for the study of eosinophilic airway inflammation such as asthma.

BAY-593 (hydrochloride) is an orally active GGTase-I inhibitor. BAY-593 (hydrochloride) can block YAP1/TAZ signaling in animals and has antitumor activity.

Prenyl-IN-1 is a protein prenylation inhibitor, especially a geranylgeranyltransferase (GGT) or a farnesyltransferase (FT) inhibitor, exhibiting potent activity against oxidative stress, and particularly in the treatment of Parkinson's Disease.