化合物GGTI-2133 T24088

Product Introduction
Bioactivity


英文名: GGTI-2133

描述: GGTI-2133 是一种有效的仿肽基香叶基转移酶 I 型抑制剂（GGTase I），IC50值为38 nM。GGTI-2133 可抑制小鼠实验性哮喘中炎症细胞向气道的侵袭。

体外活性: BSM tissues isolated from the repeatedly antigen-challenged mice were cultured for 48 h in the absence or presence of GGTI-2133. Under these conditions, the putative geranylgeranylated RhoA was decreased in a GGTI-2133 concentration-dependent manner. The in vitro incubation with GGTI-2133 also inhibited BSM hyperresponsiveness induced by antigen exposure. These findings suggest that GGTI-2133 inhibits antigen-induced BSM hyperresponsiveness, probably by reducing downstream signal transduction of RhoA.[1]

体内活性: Animals also were treated with GGTI-2133 (5 mg/kg; i.p.; once a day; mice with experimental asthma) during the antigen inhalation period. Repeated antigen inhalation caused a BSM hyperresponsiveness to acetylcholine with the increased expressions of RhoA and the anti-farnesyl-positive 21-kDa proteins, probably geranylgeranylated RhoA. The in vivo GGTI-2133 treatments significantly inhibited BSM hyperresponsiveness induced by antigen exposure.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (109.52 mM)


关键字: GGTI-2133

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相关库: Bioactive Compounds Library Max | Inhibitor Library | Bioactive Compound Library

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