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    InvivoChem Cat #: V1562
    CAS #: 1380432-32-5Purity ≥98%

    Description: EHop-016 (EHOP016; EHop 016) is a novel, potent and selective small molecule inhibitor of Rac GTPase with potential antineoplastic activity. It inhibits Rac GTPase with an IC50 of 1.1 μM for Rac1 in MDA-MB-435 and MDA-MB-231 cells, and is equally potent for inhibiting Rac3. Ehop-016 inhibited Rac activity in metastatic cancer cell MDA-MB-435 which overexpressed Rac and inhibited high endogenous Rac activity as well. It also attenuated the effects of Rac downstream protein p21-activated kinase 1 and directed migration of metastatic cancer cells. The Rho GTPase Rac regulates actin cytoskeleton reorganization to form cell surface extensions (lamellipodia) required for cell migration/invasion during cancer metastasis. Rac hyperactivation and overexpression are associated with aggressive cancers; thus, interference of the interaction of Rac with its direct upstream activators, guanine nucleotide exchange factors (GEFs), is a viable strategy for inhibiting Rac activity. 

    References: J Biol Chem. 2012 Apr 13;287(16):13228-38; J Clin Invest. 2013 Oct;123(10):4449-63. 

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    Molecular Weight (MW)430.55
    CAS No.1380432-32-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO:  86 mg/mL (199.7 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL 
    SynonymsEHOP016; EHop016; EHOP-016; EHop-016; EHOP 016; EHop 016

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    In Vitro

    In vitro activity: Rac inhibition by EHop-016 increases the activity of the closely related Rho GTPase RhoA by a compensatory mechanism. In MDA-MB-435 cells, EHop-016 (2-5 μM) inhibits association of active Vav2 with Rac1(G15A) mutant fusion protein, and reduces Rac-regulated cell functions including lamellipodia formation and cell migration. In addition, EHop-016 inhibits cell viability of MDA-MB-435 cells with IC50 of 10 μM. EHop-016 also inhibits KITD814V-induced growth in SM and AML patients-derived cells.

    Kinase Assay: Rac activity is determined from lysates of the MDA-MB-435 and MDA-MB-231 human metastatic cancer cell lines (from ATCC). Cancer cells in culture medium (DMEM, 10% FBS, pH 7.5) are treated with vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Rac1 activity is determined using the G-LISA Rac1 activation assay kit.

    Cell Assay: MDA-MB-231, MDA-MB-435, or MCF-10A mammary epithelial cells (from ATCC) are incubated in vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Cell viability is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cell survival and proliferation kit according to the manufacturer's instructions.

    In VivoTreatment of KITD814V-bearing cells with EHop-016 significantly enhances the survival of leukemic mice.
    Animal modelKITD814V-bearing mice 
    Formulation & DosageDissolved in DMSO; 2.5 μM; i.v. injection.

    J Biol Chem. 2012 Apr 13;287(16):13228-38; J Clin Invest. 2013 Oct;123(10):4449-63. 

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

    A novel Rac inhibitor, EHop-016, is a potent inhibitor of KITD814V-induced growth in SM and AML patient–derived cells. J Clin Invest. 2013 Oct;123(10):4449-63. 
    Pharmacologic inhibition of Rac GTPases delays disease progression in mice transplanted with cells bearing the KITD814V receptor. J Clin Invest. 2013 Oct;123(10):4449-63.

    Synthesis and docking of EHop-016 into the putative GEF binding pocket of Rac1.   2012 Apr 13;287(16):13228-38.


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