| S9936 |
ART558
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ART558 is a potent, selective, low molecular weight, allosteric inhibitor of DNA Polθ with an IC50 of 7.9 nM.
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Leukemia, 2025, 39(9):2152-2162
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| E1939 |
ART899
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ART899, a derivative of ART558 is a potent, specific allosteric inhibitor of DNA polymerase theta (Polθ), specifically inhibits Polθ MMEJ activity with IC50 of 180 nM. It specifically radiosensitizes tumor cells and have a potent stand-alone antitumor effect in cancer cells.
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| E1528 |
RP-6685
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RP-6685 is a potent, selective, and orally active inhibitor of DNA polymerase theta (Polθ). RP-6685 exhibits antitumor efficacy in animal models.
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Leukemia, 2025, 39(9):2152-2162
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| E1529 |
ART812
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ART812 is an orally active DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM.
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| E6541New |
PolQi2
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PolQi2 is a PolΘ inhibitor that specifically targets the N-terminal helicase domain of PolΘ, thereby suppressing alt-EJ (alternative end-joining) repair. This compound improves the accuracy and integration efficiency of gene editing across multiple loci and diverse cell lines. Additionally, PolQi2 demonstrates synergistic effects with DNA-PK inhibitors in reducing Cas9-mediated off-target activity. Its application is suitable for gene editing studies.
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