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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-DNA/RNA Synthesis-AB25583
AB25583

Chemical Structure : AB25583

CAS No.: 2565637-94-5

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AB25583 (AB 25583, AB-25583)

货号: PC-22920Not For Human Use, Lab Use Only.

AB25583 is a potent, specific small molecule inhibitor of SF2 DNA helicase domain of Polθ (Polθ-hel) with IC50 of 6 nM in Polθ-hel ATPase activity assay, selectively kills BRCA-deficient cells.

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纯度 & COA & 质检文件 纯度: 99.9% (HPLC) Select Batch:

生物&药学活性

AB25583 is a potent, specific small molecule inhibitor of SF2 DNA helicase domain of Polθ (Polθ-hel) with IC50 of 6 nM in Polθ-hel ATPase activity assay, selectively kills BRCA-deficient cells.
AB25583 shows no inhibition of WRN and RECQL5 and very minor inhibition of Bloom's (BLM) helicase.
AB25583 exhibits significantly higher potency than Novobiocin.
AB25583 shows selective killing of the BRCA2-KO cells, with little to no effect on the survival of BRCA2-WT cells, suppresses MMEJ, induces DNA damage in BRCA-deficient cells, and increases RAD51 foci in cells exposed to IR.
AB25583 exhibits synergistic activity with Olaparib in BRCA-mutant cancer cell lines.
AB25583 blocks ATPase activity of the helicase via an allosteric mechanism, inhibits Polθ-hel ATPase activity even regardless of the presence or absence of the ssDNA substrate.

物理化学性质&存储条件

分子量 452.91
分子式 C22H17ClN4O3S
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

N-(5-((4-chlorobenzyl)oxy)-1,3,4-thiadiazol-2-yl)-4-(2-methoxyphenyl)nicotinamide

参考文献

1. Ito F, et al. Nat Commun. 2024 Aug 14;15(1):7003.

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