ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC50=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 2603528-97-6
- Formula: C21H21F3N4O2
- Molecular Weight:418.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All DNA/RNA Synthesis Isoforms
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Biological Activity
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DNA Polymerase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DLD-1 | EC50 |
>12 μM
Compound: 22; ART558
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Antiproliferative activity against human DLD-1 cells
Antiproliferative activity against human DLD-1 cells
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[PMID: 36200480] |
| DLD-1 | EC50 |
0.8 nM
Compound: 22; ART558
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Antiproliferative activity against human BRCA-2 deficient DLD-1 cells
Antiproliferative activity against human BRCA-2 deficient DLD-1 cells
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[PMID: 36200480] |
| HEK293 | EC50 |
180 nM
Compound: 22; ART558
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Inhibition of microhomology-mediated end joining in HEK293 cells
Inhibition of microhomology-mediated end joining in HEK293 cells
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[PMID: 36200480] |
ART558 (GMP) (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 (GMP) (5 μM; 0-72 hours; BRCA2wild-type or BRCA2-/- cells) shows γH2AX accumulation in cells[1].
ART558 (GMP) inhibits the major Polθ mediated DNA repair process, Theta-Mediated End Joining, without targeting NonHomologous End Joining. ART558 (GMP) elicits DNA damage and synthetic lethality in BRCA1- or BRCA2-mutant tumour cells and enhances the effects of a PARP inhibitor[1].
ART558 (GMP) 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 (GMP) increases the residence time of YFP-tagged full-length Polθ at sites of laserinduced DNA damage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2603528-97-6
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Molecular Weight 418.41
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Formula C21H21F3N4O2
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SMILES
CN(C1=CC(C)=CC=C1)C([C@H]2N(C3=C(C(C(F)(F)F)=CC(C)=N3)C#N)CC[C@H]2O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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