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Medchemexpress LLC ART558 | 2603528-97-6 | 99.97% | C21H21F3N4O2 | 100 MG
SDP

Supplier:  Medchemexpress LLC HY141520100MG

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ART558 is a potent, selective, and allosteric DNA polymerase theta (Polθ) inhibitor with an IC50 of 7.9 nM. It elicits BRCA-gene synthetic lethality and DNA damage, making it suitable for cancer research, including breast cancer.

  • Elicits BRCA-gene synthetic lethality and DNA damage.
  • Inhibits Theta-Mediated End Joining without affecting Non-Homologous End Joining.
  • Enhances the effects of a PARP inhibitor.
  • Increases biomarkers of single-stranded DNA and synthetic lethality in 53BP1-defective cells.
  • Prolongs the residence time of YFP-tagged full-length Polθ at sites of laser-induced DNA damage.
  • Shows antiproliferative activity against human BRCA-2 deficient DLD-1 cells (EC50 = 0.8 nM).
  • Inhibits microhomology-mediated end joining in HEK293 cells (EC50 = 180 nM).

Catalog No. 50-003-55370


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