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EHT 1864

现货
Catalog No.
B5487
Rac家庭GTP酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,150.00
现货
10mg
¥ 1,300.00
现货
50mg
¥ 5,600.00
现货

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt581.48
Cas No.754240-09-0
FormulaC25H29Cl2F3N2O4S
Solubility≥29.05mg/mL in DMSO with gentle warming
SDFDownload SDF
Canonical SMILESFC(F)(C1=CC=C2C(SCCCCCOC3=COC(CN4CCOCC4)=CC3=O)=CC=NC2=C1)F.Cl.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

INS-1 832/13细胞(胰岛素产生细胞系)

制备方法

溶解度有限。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

1 h

实验结果

10 μM 的EHT 1864完全抑制葡萄糖刺激的胰岛素分泌(GSIS),并在10-20 mM葡萄糖存在条件下抑制GSIS。它还抑制葡萄糖诱导的膜相关Rac1和葡萄糖诱导的ERK1/2磷酸化和激活。

References:

1. Sidarala V, Veluthakal R, Syeda K, Kowluru A. EHT 1864, a small molecule inhibitor of Ras-related C3 botulinum toxin substrate 1 (Rac1), attenuates glucose-stimulated insulin secretion in pancreatic β-cells. Cell Signal. 2015 Jun;27(6):1159-67.

生物活性

描述 EHT 1864是一种有效的Rac家庭GTP酶抑制剂,作用于Rac1、Rac1b、Rac2 和Rac3,Kd值分别为40 nM、50 nM、60 nM和250 nM。
靶点 Rac1 Rac1b Rac2 Rac3    
IC50 (Kd=40 nM) (Kd=50 nM) (Kd=60 nM) (Kd=250 nM)    

质量控制

化学结构

EHT 1864