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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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Purity & Documentation Purity: >98% (HPLC)

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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