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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 dihydrochloride is a potent and novel Rac family GTPase inhibitor with Kd of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, 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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