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GGTI 2133
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GGTI 2133图片
CAS NO:191102-79-1
规格:98%
分子量:456.5
包装与价格:
包装价格(元)
500ug电议
1mg电议

产品介绍
GGTI 2133 is a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50 = 38 nM).
CAS:191102-79-1
分子式:C27H28N4O3
分子量:456.5
纯度:98%
存储:Store at -20°C

Background:

GGTI 2133 is a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50 = 38 nM). It is 140-fold selective for GGTase I over farnesyltransferase (IC50 = 5,400 nM). In vitro, it inhibits geranylgeranylation of RAP1A (IC50 = 10 uM) without inhibiting farnesylation of H-Ras (IC50 = >30 uM). 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. 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. 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).