A geranylgeranyl transferase I inhibitor (IC50 = 38 nM); 140-fold selective for GGTase I over farnesyltransferase (IC50 = 5

GGTI 2133 (trifluoroacetate salt) – 500 µg

Brand:
Cayman
CAS:
1217480-14-2
Storage:
-20
UN-No:
Non-Hazardous - /

GGTI 2133 is a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50 = 38 nM).{41574} It is 140-fold selective for GGTase I over farnesyltransferase (IC50 = 5,400 nM). In vitro, it inhibits geranylgeranylation of RAP1A (IC50 = 10 µM) without inhibiting farnesylation of H-Ras (IC50 = >30 µM). It also inhibits cell growth and decreases migration and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control values, respectively.{41575} GGTI 2133 (5 mg/kg per day, i.p.) prevents ovalbumin-induced eosinophil infiltration into airways in a mouse model of allergic bronchial asthma but does not prevent an increase in chemokines.{41576} It also blocks naloxone-induced contraction of ileum isolated from rats with morphine withdrawal syndrome and dose-dependently decreases withdrawal severity in vivo (ED50 = 0.076 mg/kg).{41577}  

 

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Description

A geranylgeranyl transferase I inhibitor (IC50 = 38 nM); 140-fold selective for GGTase I over farnesyltransferase (IC50 = 5,400 nM); inhibits geranylgeranylation of RAP1A in vitro (IC50 = 10 µM); inhibits cell growth and decreases migration and invasion of OSSC cells to 75, 45, and 27% of controls, respectively; prevents ovalbumin-induced eosinophil infiltration into airways in a mouse model of allergic bronchial asthma (5 mg/kg per day, i.p.); decreases morphine withdrawal severity in rats (ED50 = 0.076 mg/kg)

Formal name: N-[4-[(1H-imidazol-5-ylmethyl)amino]-2-(1-naphthalenyl)benzoyl]-L-leucine, 2,2,2-trifluoroacetate salt

Synonyms: 

Molecular weight: 456.5

CAS: 1217480-14-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Immunology & Inflammation|Pulmonary Diseases|Asthma||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research

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