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    VR23
    VR23

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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 #: V0695
    CAS #: 1624602-30-7Purity ≥98%

    Description: VR23 (VR-23; VR 23) is a highly potent and selective inhibitor of trypsin-like proteasome with potential antitumor activity. It inhibits trypsin-like, chymotrypsin-like, and caspase-like proteasomes with IC50s of 1 nM, 50-100 nM, and 3 μM, respectively. VR23 exhibits excellent in vivo antitumor efficacy in ATH490 athymic mice engrafted with MDA-MB-231 or RPMI 8226 cancer cells.

    References: Cancer Res. 2015 Oct 1;75(19):4164-75.

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    Molecular Weight (MW)477.88
    FormulaC19H16ClN5O6S
    CAS No.1624602-30-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 31 mg/mL (64.9 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 7-chloro-4-(4-((2,4-dinitrophenyl)sulfonyl)piperazin-1-yl)quinoline

    InChi Key: PDQVZPPIHADUOO-UHFFFAOYSA-N

    InChi Code: InChI=1S/C19H16ClN5O6S/c20-13-1-3-15-16(11-13)21-6-5-17(15)22-7-9-23(10-8-22)32(30,31)19-4-2-14(24(26)27)12-18(19)25(28)29/h1-6,11-12H,7-10H2

    SMILES Code: O=S(N1CCN(C2=CC=NC3=CC(Cl)=CC=C32)CC1)(C4=C(C=C(C=C4)[N+]([O-])=O)[N+]([O-])=O)=O

    Synonyms

    VR-23; VR 23; VR23;


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    In Vitro

    In vitro activity: In HeLa cells, VR23 induces ubiquitinated proteins accumulation. In RPMI 8226 and KAS 6 cells, VR23 inhibits cell growth with IC50 of 2.94 and 1.46 μM, respectively. VR23 is also equally effective on both bortezomib (BTZ)-sensitive and -resistant RPMI 8226 and ANBL6 cells cells. When used in combination of bortezomib in the cells above, VR23 shows synergistic effects on cell growth inhibition. In addition, VR23 selectively induces cancer cell apoptosis by causing the accumulation of ubiquitinated cyclin E.


    Kinase Assay: Exponentially growing cells on a 96-well clustered plate are treated with different concentrations of drugs or left untreated (control) for 6 hours. Proteasomes extracted with 0.5% NP40 buffer are mixed with equal amounts of samples in 100 μL total volume, and then incubated with 25 μmol/L of fluorogenic substrates (LRR- specific for trypsin-like activity, LLE-specific for caspase-like activity, and SUVY-specific for chymotrypsin-like activity) in black-bottom 96-well plates at 37°C. Fluorescence is monitored every 5 minutes at the wavelength of 360 nm (excitation) and 480 nm (emission).


    Cell Assay: Treatment with VR23 made cancer cells undergo an abnormal centrosome amplification cycle. This cycle was caused by the accumulation of ubiquitinated cyclin E. Bortezomib is clinically approved as a chymotrypsin-like proteasome inhibitor. VR23 in combinations with bortezomib, caused a synergistic effect in killing multiple myeloma cells. This synergistic effect was also effective to myeloma cells resistant to bortezomib.

    In VivoIn ATH490 athymic mice engrafted with MDA-MB-231 metastatic breast cancer cells, VR23 (30mg/kg, i.p.) shows effective antitumor and antiangiogenic activities. VR23 also reduces adverse effects caused by paclitaxel in mice.
    Animal model ATH490 athymic mice engrafted with MDA-MB-231 or RPMI 8226 cancer cells
    Formulation & DosageDissolved in 10% DMSO, 12.5% Cremophor, 12.5% ethanol, and 65% saline based diluent; 30 mg/kg; i.p. administration
    References

    Cancer Res. 2015 Oct 1;75(19):4164-75


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

     

    VR23 RELATED PROTEASOME PRODUCTS

    VR23 preferentially kills cancer over noncancer cells. Cancer Res. 2015 Oct 1;75(19):4164-75. 
     

    VR23 RELATED PROTEASOME PRODUCTS

    Combination of VR23 and bortezomib (BTZ) shows synergistic effects. Cancer Res. 2015 Oct 1;75(19):4164-75. 
     

    VR23 RELATED PROTEASOME PRODUCTS

    Localization of cyclin E to centrosomes correlates with centrosome amplification. Cancer Res. 2015 Oct 1;75(19):4164-75.  
     

    VR23 RELATED PROTEASOME PRODUCTS

    Ablation of cyclin E suppresses VR23-induced centrosome amplification. Cancer Res. 2015 Oct 1;75(19):4164-75. 
     

    VR23 RELATED PROTEASOME PRODUCTS

    Ubiquitinated cyclin E is accumulated in amplified centrosomes. Cancer Res. 2015 Oct 1;75(19):4164-75. 
     

    VR23 RELATED PROTEASOME PRODUCTS

    VR23 shows anticancer and antiangiogenesis activities. Cancer Res. 2015 Oct 1;75(19):4164-75. 


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