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ART558

Cat. No. M21168

All AbMole products are for research use only, cannot be used for human consumption.

ART558 Structure
Synonym:

ART-558

Size Price Availability Quantity
1mg USD 150 In stock
2mg USD 240 In stock
5mg USD 390 In stock
10mg USD 580 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
References

[1] Joost Schimmel, et al. Cell Rep. Modulating mutational outcomes and improving precise gene editing at CRISPR-Cas9-induced breaks by chemical inhibition of end-joining pathways

[2] Gonzalo Rodriguez-Berriguete, et al. Clin Cancer Res. Small-molecule Polθ inhibitors provide safe and effective tumor radiosensitization in preclinical models

[3] Martin L Stockley, et al. J Med Chem. Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta

[4] Diana Zatreanu, et al. Nat Commun. Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance

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Keywords: ART558, ART-558 supplier, DNA/RNA Synthesis, inhibitors, activators

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