ART558

SKU: orb1298221

Description

ART558

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 2603528-97-6
• MW: 418.41
• Purity: 99.18% (May vary between batches)
• Formula: C₂₁H₂₁F₃N₄O₂
• SMILES: CN(C(=O)[C@@H]1[C@H](O)CCN1c1nc(C)cc(c1C#N)C(F)(F)F)c1cccc(C)c1
• Target: DNA/RNA Synthesis
• Solubility: 10% DMSO+90% Corn Oil:4 mg/mL (9.56 mM);DMSO:45 mg/mL (107.55 mM)

Bioactivity

• Target IC50:
  DNA polymerase Polθ (POLQ):7.9 nM
• In Vitro:
  ART558 (5μM; 0~72 hours; BRCA2wild-type or BRCA2‒/‒ cells) shows γH2AX accumulation in cells. 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. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DNA polymerase, DNA Synthesis, DNASynthesis, ART 558, ART558, ART-558, RNA Synthesis, RNASynthesis

Compound Identifiers

PubChem CID

156068882