Chemical Structure : Thymine DNA glycosylase inhibitor C-271
CAS No.:
3092641-80-7
Thymine DNA glycosylase inhibitor C-271
货号: PC-25978Not For Human Use, Lab Use Only.
C-271 is a first-in-class, specific small-molecule inhibitor of Thymine DNA glycosylase (TDG), inhibits TDG's glycosylase activity with similar efficacy across different substrates with IC50 of 0.16-0.25 uM, covalently targets TDG at C276.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
C-271 is a first-in-class, specific small-molecule inhibitor of Thymine DNA glycosylase (TDG), inhibits TDG's glycosylase activity with similar efficacy across different substrates with IC50 of 0.16-0.25 uM, covalently targets TDG at C276.
C-271 specifically binds to TDG with a high-affinity association constant (Ka= 1.46 uM), but does not bind to other primary human glycosylase homologs (for example, UNG2 and NEIL1) or APE1 (apurinic/apyrimidinic endonuclease 1), which functions downstream of TDG in the BER.
C-271 interferes with TDG's DNA binding, thereby inhibiting its glycosylase activity.
C-271 suppresses p53-deficient tumors growth and induces cytoplasmic dsRNA accumulation in p53-deficient tumor cells.
TDG inhibition via C-271 in p53-deficient cancer cells leads to DHX9 downregulation and, thus, aberrant dsRNA accumulation, which activates the RIG-I/MDA5-MAVS sensing pathway, resulting in tumor suppression and enhanced antitumor immunity.
物理化学性质&存储条件
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分子量
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234.25
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分子式
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C13H14O4
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-(4-hydroxy-2-methoxy-5-methylphenyl)-3-oxabicyclo[3.1.0]hexan-2-one
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参考文献
1. Zhou JX, et al. Nat Chem Biol. 2026 Jan 22. doi: 10.1038/s41589-025-02100-1.
