2603528-97-6
2603528-97-6 structure
- Name: ART558
- Chemical Name: ART558
- CAS Number: 2603528-97-6
- Molecular Formula: C21H21F3N4O2
- Molecular Weight: 418.41
- Catalog: Research Areas Cancer
- Create Date: 2021-09-14 15:01:53
- Modify Date: 2025-08-25 16:20:19
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ART558 is a nanomolar potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer[1].
| Name | ART558 |
|---|
| Description | ART558 is a nanomolar potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer[1]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 7.9 nM (Polθ)[1] |
| In Vitro | ART558 (0~10 μM; 7 days; BRCA2wild-type or BRCA2‒/‒ cells) shows synthetic lethality and a combinatorial effect with the PARPi olaparib in previously described isogenic models of BRCA1-deficiency[1]. ART558 (5μM; 0~72 hours; BRCA2wild-type or BRCA2‒/‒ cells) shows γH2AX accumulation in cells[1]. ART558 inhibits the major Polθ mediated DNA repair process, Theta-Mediated End Joining, without targeting NonHomologous End Joining. 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[1]. Cell Viability Assay[1] Cell Line: BRCA2wild-type or BRCA2‒/‒ cells Concentration: 0~10 μM Incubation Time: 7 days Result: Showed synthetic lethality and a combinatorial effect with the PARPi olaparib in previously described isogenic models of BRCA1-deficiency. Western Blot Analysis[1] Cell Line: BRCA2wild-type or BRCA2‒/‒ cells Concentration: 5μM Incubation Time: 0~72 hours Result: Showed γH2AX accumulation in cells. |
| References |
| Molecular Formula | C21H21F3N4O2 |
|---|---|
| Molecular Weight | 418.41 |