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PVZB3001

Chemical Structure : PVZB3001

CAS No.: 103386-74-9

PVZB3001 (PVZB 3001)

Catalog No.: PC-49660Not For Human Use, Lab Use Only.

PVZB3001 (PVZB 3001) is a selective and cell-permeable dual inhibitor of IDO1 and TDO with IC50 value of 0.62 μM for rhTDO and 1.71 μM for rhIDO1, respectively.

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    Biological Activity

    PVZB3001 (PVZB 3001) is a selective and cell-permeable dual inhibitor of IDO1 and TDO with IC50 value of 0.62 μM for rhTDO and 1.71 μM for rhIDO1, respectively.
    PVZB3001 inhibited cellular Kyn production dose-dependently in A172 cells and in A431 cells upon IFN-γ stimulation, with an IC50 value of 0.96 μM in A172 cells and 0.74 μM in A431 cells.
    PVZB3001 showed competitive inhibition against TDO.
    PVZB3001 recovered NK cell viability and function by inhibiting Kyn accumulation in conditioned medium of both IDO1- and TDO-expressing cells.
    PVZB3001 suppressed the growth of tumor in a dose-dependent manner without body weight loss, especially showed significant antitumor effect when treated with 25.0 mg/kg (oral) and with 50.0 mg/kg (oral) respectively.

    Physicochemical Properties

    M.Wt 254.37
    Formula C10H14N4S2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    1,2-phenylenebis(methylene) dicarbamimidothioate

    References

    1. Saeko Yoshioka, et al. Int J Tryptophan Res. 2022 Nov 30;15:11786469221138456.

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