Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 163.00 | |
5 mg | In stock | $ 413.00 | |
10 mg | In stock | $ 618.00 | |
25 mg | In stock | $ 985.00 | |
50 mg | In stock | $ 1,330.00 | |
100 mg | In stock | $ 1,790.00 |
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]. |
Molecular Weight | 418.41 |
Formula | C21H21F3N4O2 |
CAS No. | 2603528-97-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 150 mg/mL (358.5 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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ART558 2603528-97-6 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis ART 558 ART-558 inhibitor inhibit