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NSC232003
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NSC232003图片
CAS NO:1905453-18-0
包装与价格:
包装价格(元)
10mM (in 1mL Water)电议
1mg电议
5mg电议
50mg电议
100mg电议

产品介绍

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。

Cas No.1905453-18-0
Canonical SMILESO=C1NC(/C(C=N1)=C(NO)/C)=O
分子式C6H7N3O3
分子量169.14
溶解度Water : 17 mg/mL (100.51 mM);DMSO :< 1 mg/mL (insoluble or slightly soluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.

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 pKa 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[1].

[1]. Myrianthopoulos V, et al. Tandem virtual screening targeting the SRA domain of UHRF1 identifies a novel chemical tool modulating DNA methylation. Eur J Med Chem. 2016 May 23;114:390-6.