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EHT 1864
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。
EHT 1864图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
EHT 1864 是 Rac 家族小 GTPase 的抑制剂。

Cell lines

INS-1 832/13 cells (Insulin-Producing-Cell Line)

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

1 h

Applications

10 μM EHT 1864 shows a complete inhibition of GSIS (Glucose-stimulated insulin secretion)and inhibits GSIS at 10-20mM glucose. It also suppresses a glucose-induced membrane association of Rac1 and glucose-induced ERK1/2 phosphorylation and activation.

产品描述

EHT 1864 is a small-molecule inhibitor of Rac family small GTPases with Kd value of 40nM for Rac1 [1].

In NIH 3T3 mouse fibroblasts, EHT 1864 treatment shows an 80% reduction in PDGF-induced lamellipodia formation. EHT 1864 at concentration of 50μM can completely inhibit the complex formation between Rac1 and PAK-RBD and cause the release of nucleotide from Rac1. The reassociation of nucleotide with Rac1 induced by EDTA or the Tiam1 can also be blocked by EHT 1864. EHT 1864 is most potent to Rac1, both in the binding affinity and stimulation of nucleotide release. It binds to Rac1b, Rac2 and Rac3 with Kd values of 50nM, 60nM and 250nM, respectively. Moreover, EHT 1864 can suppress cellular transformation induced by Rac1 with an 80% inhibition of focus-forming activity [1].

References:
[1] Shutes A, Onesto C, Picard V, et al. Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. Journal of Biological Chemistry, 2007, 282(49): 35666-35678.