| Name | ART558 |
| Description | ART558 is a 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. |
| 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[1]. |
| Storage | Keep away from direct sunlight,Keep away from moisture,
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+90% Corn Oil : 4 mg/mL (9.56 mM), Sonication is recommended.
DMSO : 45 mg/mL (107.55 mM), Sonication is recommended.
|
| Keywords | RNASynthesis | RNA Synthesis | DNASynthesis | DNA Synthesis | DNA polymerase | ART-558 | ART558 | ART 558 |
| Inhibitors Related | 5-Fluorouracil | Adenine hemisulfate | Erythromycin thiocyanate | Guanidine hydrochloride | Hexane-1,6-diol | 1,4-Naphthoquinone | Adenine | Vidarabine | Carbazole | Thymidine | Docosanoic acid | Usnic Acid |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Cell Cycle Compound Library | Covalent Inhibitor Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
