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    EHT 1864 2HCl
    EHT 1864 2HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1566
    CAS #: 754240-09-0Purity ≥98%

    Description: 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. 

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

    Related CAS#: CAS#754240-09-0 (dihydrochloride); 754239-64-0 (free base) 

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    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


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    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.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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