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ART558 is a nanomolar, highly potent, selective, low-molecular-weight, variant DNA polymerase active Polθ inhibitor (IC50=7.9 nM). ART558 elicits DNA damage and synthetic lethality in BRCA1- or BRCA2-mutant tumour cells and enhances the effects of a PARP inhibitor. ART558 increases biomarkers of single-stranded DNA and synthetic lethality in 53BP1-defective cells whilst the inhibition of DNA nucleases that promote end-resection reversed these effects, implicating these in the synthetic lethal mechanism-of-action. ART558 increases the residence time of YFP-tagged full-length Polθ at sites of laserinduced DNA damage. ART558 can be used in cancer research.
| Molecular Weight | 418.41 |
| Formula | C21H21F3N4O2 |
| CAS Number | 2603528-97-6 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage | 2-8°C, protect from light, dry, sealed |
| Related DNA/RNA Synthesis Products |
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