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ART558 

Cat. No.: HY-141520
Handling Instructions

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.

For research use only. We do not sell to patients.

ART558 Chemical Structure

ART558 Chemical Structure

CAS No. : 2603528-97-6

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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].

IC50 & 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

418.41

Formula

C₂₁H₂₁F₃N₄O₂

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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ART558
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