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Thymidylate synthase destabilizer E7

Chemical Structure : Thymidylate synthase destabilizer E7

CAS No.:

Thymidylate synthase destabilizer E7

Catalog No.: PC-49578Not For Human Use, Lab Use Only.

Thymidylate synthase destabilizer E7 is a small molecule human thymidylate synthase (hTS) destabilizer, binds at the monomer-monomer interface and shifts the dimerization equilibrium of both the recombinant and the intracellular protein toward the inactive monomers.

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    Biological Activity

    Thymidylate synthase destabilizer E7 is a small molecule human thymidylate synthase (hTS) destabilizer, binds at the monomer-monomer interface and shifts the dimerization equilibrium of both the recombinant and the intracellular protein toward the inactive monomers.
    E7 induced apoptosis in cancer cells and a decrease of hTS levels due to enhanced proteasomal degradation of the enzyme monomers with respect to the dimers.
    E7 caused a higher reduction of cancer growth and had lower toxicity than 5-fluorouracil (5-FU), the prodrug of 5-FdUMP, in a mouse model of orthotopic pancreatic cancer.

    Physicochemical Properties

    M.Wt 499.57
    Formula C22H17N3O5S3
    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

    phenyl[2-(4-nitrophenylthio)-N-(6-methanesulfonylbenzothiazol-2-yl)]acetamide

    References

    1. Costantino L, et al. Elife. 2022 Dec 7;11:e73862.

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