化合物ART558 T9275

Product Introduction
Bioactivity


英文名: ART558

描述: ART558 是一种高效的、选择性的、变构 DNA 聚合酶活性的 Polθ 抑制剂，IC50为7.9 nM。ART558 可用于癌症研究。

体外活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (107.55 mM)


关键字: ART 558 | ART558 | ART-558

相关产品: DMT-dU-CE Phosphoramidite | Gemcitabine hydrochloride | Adenine hydrochloride | Dmt-2'fluoro-da(bz) amidite | YK-4-279 | Dihydromyricetin | RdRP-IN-6 | 6-Mercaptopurine hydrate | Favipiravir | Farudodstat

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Active Compound Library | DNA Damage & Repair Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途