Drug intelligence / Profile preview

LC0296

Development stage
Preclinical
Lead developer
University of Minnesota
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

LC0296 (also known as LC-0296) is a selective small molecule inhibitor of sirtuin 3 (SIRT3) with an IC50 of 3.6 µM, demonstrating approximately 20-fold and 10-fold selectivity over SIRT1 and SIRT2, respectively. Developed by researchers at the University of Minnesota, LC0296 acts as an epigenetic modulator that increases mitochondrial protein acetylation, elevates reactive oxygen species (ROS) levels, and impairs mitochondrial adaptation. In preclinical studies, LC0296 has shown antiproliferative and proapoptotic activity in head and neck squamous cell carcinoma (HNSCC) and oral squamous cell carcinoma (OSCC) cells, and has been found to sensitize breast cancer cells to endocrine therapies such as fulvestrant.

Other names
(S)-methyl 2-(((benzyloxy)carbonyl)amino)-5-((1-(3-carbamoylbenzyl)-1H-indol-4-yl)amino)-5-oxopentanoatemethyl N2-((benzyloxy)carbonyl)-N5-(1-(3-carbamoylbenzyl)-1H-indol-4-yl)-L-glutaminate
02

Targets

SIRT2 (NAD-dependent protein deacetylase sirtuin-2)SIRT1 (NAD-dependent protein deacetylase sirtuin-1)SIRT3 (NAD-dependent protein deacetylase sirtuin-3)

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