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    VER155008
    VER155008

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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 #: V0879
    CAS #: 1134156-31-2Purity ≥98%

    Description: VER-155008 (VER 155008; VER155008) is an HSP70 (heat shock protein 70) inhibitor with anti-AD (alzheimer's disease) effects. It inhibits HSP70, HSC70 (Heat shock cognate 70), and GRP78 with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays, respectively, and exhibits >100-fold selectivity for HSP70 over HSP90. VER-155008 significantly promoted axonal regrowth in amyloid β-treated neurons in vitro and improved object recognition, location, and episodic-like memory in 5XFAD mice. HSC70 may be used as a new therapeutic target for AD treatment.

    References:  2018 Jan 30;9:48;  2010 Aug;66(3):535-45.

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    • 香港大学
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    Molecular Weight (MW)556.40
    FormulaC25H23Cl2N7O4 
    CAS No.1134156-31-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 93 mg/mL (199.0 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)1% CMC+0.5% Tween-80: 30 mg/mL
    SynonymsVER 155008; VER155008; VER-155008; 

    Chemical Name: 5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine

    SMILES Code: O[[email protected]@H]([[email protected]]([[email protected]](N1C(NCC2=CC=C(Cl)C(Cl)=C2)=NC3=C(N=CN=C31)N)O4)O)[[email protected]]4COCC5=CC=C(C#N)C=C5


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    In Vitro

    In vitro activity: VER-155008 is a potent inhibitor of HSP70 family with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70 (Heat shock cognate 70), and GRP78, respectively, it has >100-fold selectivity over HSP90. VER 155008 has been shown to contribute to cancer cell survival via anti-apoptotic functions, that inhibits Hsp70 with IC50 of 0.5 μM as well as heat shock cognate 71 kDa protein (Hsc70) and 78 kDa glucose-regulated protein (Grp78) but to a lesser extent. VER-155008 significantly promoted axonal regrowth in amyloid β-treated neurons in vitro and improved object recognition, location, and episodic-like memory in 5XFAD mice. Furthermore, VER-155008 penetrated into the brain after intraperitoneal administration, suggesting that VER-155008 acts in the brain in situ. Immunohistochemistry revealed that VER-155008 reduced bulb-like axonal swelling in the amyloid plaques in the perirhinal cortex and CA1 in 5XFAD mice, indicating that VER-155008 also reverses axonal degeneration in vivo. Moreover, the two main pathological features of AD, amyloid plaques and paired helical filament tau accumulation, were reduced by VER-155008 administration in 5XFAD mice. This is the first report to show that the inhibition of HSC70 function may be critical for axonal regeneration and AD-like symptom reversal. This study provides evidence that HSC70 can be used as a new therapeutic target for AD treatment.

    Kinase Assay: VER-155008 is a potent inhibitor of HSP70 family with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70 (Heat shock cognate 70), and GRP78, respectively, it has >100-fold selectivity over HSP90. VER 155008 has been shown to contribute to cancer cell survival via anti-apoptotic functions, that inhibits Hsp70 with IC50 of 0.5 μM as well as heat shock cognate 71 kDa protein (Hsc70) and 78 kDa glucose-regulated protein (Grp78) but to a lesser extent. 


    Cell Assay: Embryos are removed from a pregnant ddY mouse at 14 days of gestation. Cells are treated with or without 10 μM Aβ25-35 for 3 days, followed by the addition of 0.05, 0.5, or 5 μM VER-155008 or vehicle solution (0.1% DMSO) for 4 days. The Aβ25-35 is incubated at 37°C for 4 days prior to treatment to facilitate aggregation. The cells are fixed with 4% paraformaldehyde and immunostained at 4°C for 24 h with antibodies against the axonal marker, mouse phosphorylated neurofilament heavy subunit, and against the neuronal marker, rabbit microtubule-associated protein 2. Alexa Fluor 488-conjugated goat anti-mouse IgG (1:400) and Alexa Fluor 568-conjugated goat anti-rabbit IgG (1:400) are used as secondary antibodies. Fluorescence images (864.98 μm × 645.62 μm) are captured using a fluorescence microscopy system. The lengths of the pNF-H-positive axons are measured using MetaMorph version 7.8

    In VivoVER-155008 (25 mg/kg, i.v.) exhibits plasma clearance in naive female BALB/c mice. VER-155008 (40 mg/kg, i.v.) also shows rapid plasma clearance, and reduces the tumor levels in the HCT116 tumor bearing nude BALB/c mice[1]. VER-155008 (10 μmol/kg/day, i.p.) rescues memory deficits, and reduces axonal swelling associated with amyloid plaques in 5XFAD mice. VER-155008 (89.9 μmol/kg/day, i.p.) penetrates into the brain after administration in 5XFAD mice. VER-155008 also decreases amyloid plaques and PHF-tau associated with amyloid plaques in 5XFAD mice.
    Animal modelBALB/c mice
    Formulation & Dosage

    Formulation method 1: VER-155008 was dissolved in 10% dimethyl sulfoxide (DMSO)-containing saline and administered intraperitoneally (10 mmol/kg/day) to 5XFAD mice for 18 days. [1]

    Formulation method 2: Female BALB/c mice were dosed intravenously with 25 mg/kg VER-155008 into the lateral tail vein as a solution in 10% DMSO/5% Tween 80/85% saline (v/v/v). [2]

    References

    [1].  2018 Jan 30;9:48

    [2].  2010 Aug;66(3):535-45.


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

     

    VER155008

    VER-155008 administration rescued memory deficits in 5XFAD mice. 2018 Jan 30;9:48.

     

    VER155008

    VER-155008 penetrates into the brain after intraperitoneal administration in 5XFAD mice.  2018 Jan 30;9:48.

     

    VER155008

    VER-155008 administration reduced axonal swelling associated with amyloid plaques in 5XFAD mice.  2018 Jan 30;9:48.

     

    VER155008

    VER-155008 treatment reversed Aβ-induced axonal degeneration in cultured neurons.  2018 Jan 30;9:48.

     

    VER155008

    VER-155008 administration reduced axonal swelling associated with amyloid plaques in 5XFAD mice.  2018 Jan 30;9:48.
     

    VER155008

    VER-155008 administration reduced amyloid plaques in 5XFAD mice. Aβ1-40/42 was visualized by immunostaining in the perirhinal cortex and hippocampal CA1. (A) Representative images of Aβ1-40/42-positive amyloid plaques in the perirhinal cortex are shown. The amyloid plaques are indicated with white arrowheads.  2018 Jan 30;9:48.


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