1905453-18-0

中文名称:

1905453-18-0

中文同义词:

UHRF1抑制剂(NSC232003)

英文名称:

NSC232003

英文同义词:

NSC232003

CAS号:

1905453-18-0

分子式:

C6H7N3O3

分子量:

169.14

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1905453-18-0.mol

生物活性

NSC232003 是一种高效的可渗透细胞的 UHRF1 抑制剂，可抑制 DNA 甲基化，并破坏 DNMT1/UHRF1 相互作用。

靶点

UHRF1

体外研究

NSC232003, a uracil derivative freely available by the NCI/DTP repository, provides a versatile lead for developing highly potent and cell-permeable UHRF1 inhibitors that will enable dissection of DNA methylation inheritance. NSC232003 is indeed an effective DNA methylation inhibitor and indicate that this particular nucleotide scaffold could provide a versatile basis for the design of potent UHRF1 inhibitors. NSC232003 is predicted to be partially deprotonated at pH 7, as the pK a of the more acidic imide nitrogen of the pyrimidine ring is a value of 7.6 in NSC232003. The DNMT1/UHRF1 interactions are significantly reduced after 4 h of incubation of U251 glioma cells with the most potent compound NSC232003, showing a 50% interaction inhibition at 15 μM as well as induction of global DNA cytosine demethylation as measured by ELISA.