EHT 1864
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EHT 1864是Rac家族GTP酶的小分子抑制剂,对Rac1的作用最强,无论是结合亲和力还是刺激核苷酸的释放。作用于Rac1、Rac1b、Rac2 和Rac3,Kd值分别为40 nM、50 nM、60 nM和250 nM[1]。
在NIH 3T3小鼠成纤维细胞中,EHT 1864减少了80%的PDGF诱导的伪足的形成。EHT 1864在50μM浓度时可以完全抑制Rac1和PAK-RBD复合体的形成,导致核苷酸从Rac1的释放。EHT 1864也可以抑制EDTA或Tiam1诱导的核苷酸与Rac1的重新关联。而且,EHT 1864可以抑制Rac1诱导的细胞转化,并抑制了80%的集落形成活性[1]。
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 581.48 |
Cas No. | 754240-09-0 |
Formula | C25H29Cl2F3N2O4S |
Solubility | ≥29.05 mg/mL in DMSO with gentle warming; ≥16.53 mg/mL in H2O; ≥2.1 mg/mL in EtOH with gentle warming and ultrasonic |
SDF | Download SDF |
Canonical SMILES | FC(F)(C1=CC=C2C(SCCCCCOC3=COC(CN4CCOCC4)=CC3=O)=CC=NC2=C1)F.Cl.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
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) |
质量控制和MSDS
- 批次:
化学结构
![EHT 1864](http://www.apexbt.com/media/diy/images/struct/B5487.png)
相关生物数据
![EHT 1864 EHT 1864](/media/diy/images/wb/B5487_1.jpg)