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EHT 1864 2HCl
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 2HCl图片
CAS NO:754240-09-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
EHT 1864 2HCl (EHT-1864; EHT1864), the dihydrochloride salt of EHT-1864, is a potent and novel Rac family GTPase inhibitor with important biological activity. It inhibits Rac1, Rac1b, Rac2 and Rac3 with Kd values of 40 nM, 50 nM, 60 nM and 250 nM, respectively. EHT 1864 attenuates glucose-stimulated insulin secretion in pancreatic β-cells. EHT 1864 specifically inhibits glucose-induced Rac1 activation and membrane association and associated downstream signaling events culminating in inhibition of GSIS.
理化性质和储存条件
Molecular Weight (MW)581.47
FormulaC25H29Cl2F3N2O4S
CAS No.754240-09-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (172.0 mM)
Water: 100 mg/mL (172.0 mM)
Ethanol: <1 mg/mL
SMILESO=C1C=C(CN2CCOCC2)OC=C1OCCCCCSC3=CC=NC4=CC(C(F)(F)F)=CC=C34
SynonymsEHT-1864; EHT1864; EHT 1864 HCl
实验参考方法
In Vitro

In vitro activity: EHT 1864 selectively inhibits Rac-induced lamellipodia formation, and specifically reverses cell transformation induced by constitutively activated mutants of Rac1 and Tiam1. EHT 1864 strongly impaires oncogenic Ras-induced cell proliferation in NIH 3T3 cells stably expressing H-Ras(61L) protein. EHT 1864 also reduces both extracellular and intracellular levels of Aβ peptides by inhibiting the γ-secretase-dependent cleavage of APP. In cultured hippocampal pyramidal neurons, EHT 1864, via inhibition of Rac1, rescues the phenotype induced by Rich2 knock-down.


Kinase Assay: For inhibitor:GTPase binding analyses, aliquots of small GTPase solution (containing 1 μM inhibitor) are titrated into a solution of 1 μM inhibitor in the cuvette. Changes in fluorescence anisotropy are monitored at λex = 360 nm, λem = 440 nm, 30 s after each addition. All data analysis and curve fitting were performed using Microsoft Excel and QuantumSoft's ProFit for Mac OS X.


Cell Assay: NIH 3T3 cells stably expressing oncogenic Ras are plated in 96-well plates. The cells are cultured for up to 4 days in complete growth medium, either alone, or supplemented with 5 μM EHT 1864. Cell growth is then assessed using the conversion of MTT to a formazan product. Briefly, the MTT reagent (from a 5 mg/ml solution diluted in PBS) is added to the wells at a final concentration of 0.5 mg/ml, and the cells are further incubated for 4 h at 37°C. The medium is then removed, and the reaction is terminated by adding 100 μl/well Me2SO. The absorbance is read at 570 nm using a microplate reader.

In VivoEHT 1864 (40 mg/kg i.p.) significantly reduces Abeta 40 and Abeta 42 levels in guinea pig brains.
Animal modelMale Hartley albino guinea pigs
Formulation & DosageDissolved in saline; 40 mg/kg daily; i.p. injection
References

J Biol Chem. 2007 Dec 7;282(49):35666-78; J Biol Chem. 2005 Nov 11;280(45):37516-25.