Drug intelligence / Profile preview

NSC232005

Development stage
Preclinical
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
In Vitro
01

Overview

NSC232005 is a small molecule **uracil derivative** bearing an exocyclic primary aliphatic amine. It acts as a selective inhibitor that binds to the SRA (Set and Ring Associated) domain of **UHRF1**, a protein involved in the recognition of hemimethylated DNA and recruitment of DNA methyltransferase 1 (DNMT1) for maintenance methylation. Inhibition of UHRF1 by NSC232005 disrupts DNA methylation processes, leading to reduced maintenance methylation in cancer cells, particularly demonstrated in HCT116 colorectal cancer cells. Treatment with NSC232005 leads to a significant decrease in DNA methylation levels selectively in malignant cells with little effect on healthy hematopoietic cells, suggesting a degree of cancer cell specificity. NSC232005 is supplied by the NCI/DTP (National Cancer Institute Developmental Therapeutics Program). Its mechanism and selectivity profile make it a promising lead compound for further development as a targeted **epigenetic modulator** for oncology applications[1][3][5].

02

Targets

UHRF1

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