Drug intelligence / Profile preview

NCT-501

Development stage
Preclinical
Lead developer
National Center for Advancing Translational Sciences
Modality
Small Molecules
Administration
Oral, Intravenous, Intraperitoneal, Intratumoral
01

Overview

NCT-501 is a potent and selective small molecule inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1), an enzyme frequently overexpressed in cancer stem cells (CSCs) and associated with therapeutic resistance. Developed by the National Center for Advancing Translational Sciences (NCATS) as a chemical probe, NCT-501 exhibits an IC50 of approximately 40 nM and demonstrates high selectivity (over 100-fold) for ALDH1A1 compared to other ALDH isoforms such as ALDH1A2, ALDH1A3, and ALDH2. In preclinical studies, particularly in glioblastoma models, NCT-501 has been shown to reduce cell mobility, reverse mesenchymal differentiation, and sensitize tumor cells to chemotherapy agents like temozolomide. It serves as a valuable research tool for investigating the role of ALDH1A1 in tumor progression, stemness, and the modulation of TGF-β signaling.

Other names
ALDH1A1 inhibitor NCT-501ALDH-1A1 inhibitor NCT-501ALDH 1A1 inhibitor NCT-501
02

Targets

HSD17B4 (17-beta-hydroxysteroid dehydrogenase type 4)ALDH1B1 (Aldehyde dehydrogenase 1B1)ALDH2 (Mitochondrial Aldehyde Dehydrogenase)ALDH3A1 (Aldehyde dehydrogenase 3 family member A1)HPGD (15-hydroxyprostaglandin dehydrogenase)

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