ART5537 | EXO1 inhibitor | Probechem Biochemicals

Chemical Structure : ART5537

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ART5537 (ART-5537)

货号: PC-26135Not For Human Use, Lab Use Only.

ART5537 (ART-5537) is highly potent and selective inhibitor of Exonuclease 1 (EXO1) with IC50 of 3.4 nM, inhibits homologous recombination (HR) with EC50 of 7.2 nM in HR reporter assays.

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生物&药学活性

ART5537 (ART-5537) is highly potent and selective inhibitor of Exonuclease 1 (EXO1) with IC50 of 3.4 nM, inhibits homologous recombination (HR) with EC50 of 7.2 nM in HR reporter assays.
ART5537 direcly binds to EXO1 with SPR KD of 6.8 nM.
ART5537 displays ≥200-fold selectivity over a panel of the wider nuclease superfamily, including DNA2, MRE11, MUS81, SNM1A etc.
ART5537 displays unambiguous dose-dependent cellular target engagement with an EC50 of 55 nM.
ART5537 kills MDA-MB-436 and HCC1937 (BRCA1 null), SUM149PT (BRCA1 Δ11q hypomorph), and HCC38 (BRCA1 promoter methylated) breast cancer cells in the low micromolar range, exhibits strong sensitization to ionizing radiation (IR) in HCT116 cells.

物理化学性质&存储条件

分子量	447.88
分子式	C23H18ClN5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-1-(4-Chloro-2,7-naphthyridin-1-yl)-5-hydroxy-3-(1-phenylethyl)-2,3-dihydro-1H-pyrido[2,1-f][1,2,4]triazine-4,6-dione

参考文献

1. Sam E Mann, et al. J Med Chem. 2025 Dec 25;68(24):26432-26447.

ART5537 (ART-5537)

生物&药学活性

物理化学性质&存储条件

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ART5537 (ART-5537)

生物&药学活性

物理化学性质&存储条件

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