Drug intelligence / Profile preview

BAS-2

Development stage
Preclinical
Lead developer
RCSI University of Medicine and Health Sciences
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

BAS-2 is a selective, mechanism-based small molecule inhibitor of histone deacetylase 6 (HDAC6) with a unique isothiouronium core. Discovered through a phenotypic small-molecule screen targeting triple-negative breast cancer (TNBC) cells, BAS-2 selectively kills cancer cells independent of mitochondrial apoptosis. It acts as a prodrug that undergoes intracellular hydrolysis to generate a mercaptoacetamide active species, which directly coordinates with the catalytic zinc ion of human HDAC6. BAS-2 has been shown to reduce glycolytic metabolism, alter mitochondrial cristae structure, and inhibit tumor cell migration, invasion, and spheroid formation in TNBC models.

Other names
2-[(3a,4,5,6,7,7a-hexahydro-1H-benzimidazol-2-yl)thio]-1-(4-morpholinyl)-ethanone2-(3a,4,5,6,7,7a-hexahydro-1H-1,3-benzodiazol-2-ylsulfanyl)-1-(morpholin-4-yl)ethan-1-oneMCULE-7388843487MCULE7388843487MCULE 7388843487
02

Targets

HDAC6 (Histone deacetylase 6)

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