您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > RBC8
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
RBC8
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。
RBC8图片
CAS NO:361185-42-4
规格:98%
分子量:424.45
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
Ral GTPase inhibitor
CAS:361185-42-4
分子式:C25H20N4O3
分子量:424.45
纯度:98%
存储:Store at -20°C

Background:

RBC8 inhibit Ral GTPase with IC50 values of 3.5 μM and 3.4 μM in Ral-dependent lines H2122 and H358 [1].


RalA and B are Ras-like GTPases. They are important drivers of metastasis and tumor growth [1].


RBC8 reduced the activation of RalA in living cells. Ral is required for spreading murine embryonic fibroblasts (MEFs) and lipid raft exocytosis on fibronectin-coated cover slips. In these cells, the spreading of WT MEFs was inhibited by the depletion of RalA via siRNA, whereas caveolin deficient (Cav1-/-) MEFs were resistant to RalA depletion. Treatment with RBC8 inhibited only the cell spreading in the WT MEFs, it did not inhibited the cell spreading in Cav1-/- MEFs. A Ral pull-down assay showed that RBC8 inhibited the activation of both RalA and RalB in both the H2122 and H358 cell lines. In H2122 and H358 cells with Ral knockdown by siRNA, treatment with RBC8 did not show further inhibition of colony formation [1].


In nude mice inoculated with H2122 human lung cancer cells subcutaneously, treatment with RBC8 at 50 mg/kg/d for 21 days (except weekends) intraperitoneally showed an inhibitory effect on tumor growth to a similar extent as dual knockdown of RalA and B. H358 is a lung cancer line. In this cell line, similar results were yielded [1].


Reference:
[1].  Yan C, Liu D, Li L, et al. Discovery and characterization of small molecules that target the Ral GTPase. Nature, 2014, 515(7527): 443-447.