ART558

Based on 11 reference(s) in Google Scholar 8 10 11

Axon 4355

CAS [2603528-97-6]

MF C21H21F3N4O2
MW 418.41

  • Purity: 99%
  • Optical purity: 100% e.e.
  • Soluble in DMSO and EtOH
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ART558

Description

ART558 is a highly potent, selective allosteric inhibitor of the polymerase function of DNA polymerase Polθ (IC50 value of 7.9 nM). ART558 inhibits the major Polθ-mediated DNA repair process, Theta-Mediated End Joining, without targeting Non-Homologous End Joining. In addition, ART558 elicits DNA damage and synthetic lethality in BRCA1- or BRCA2-mutant tumour cells and enhances the effects of a PARP inhibitor.

KEYWORDS: ART558 | Supplier | Polθ inhibitor | ART 558 | ART-558 | CAS [2603528-97-6] | DNA-RNA | DNA | Inhibitor | Enzymes | PARP inhibitor resistance

Highly potent, selective allosteric Polθ inhibitor

Chemical name

N-Methyl-N-1,3-tolyl-(2S,3R)-1-(3-cyano-6-methyl-4-(trifluoromethyl)-2-pyridyl)-3-hydroxy-2-pyrrolidinecarboxamide

Parent CAS No.

[2603528-97-6]

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5 mg €180.00 In Stock
25 mg €700.00 In Stock
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2 x 5 mg €320.00 In Stock
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The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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