Drug intelligence / Profile preview

VAS3947

Development stage
Preclinical
Lead developer
University of Salerno
Modality
Small Molecules
Administration
Intravenous, Intraperitoneal
01

Overview

**VAS3947** is a small molecule compound primarily investigated as a pan-NADPH oxidase (NOX) inhibitor. It is structurally related to VAS2870 but with improved solubility and similar inhibitory profile for various NOX isoforms[3][1][5]. VAS3947 inhibits NOX activity, thus interfering with reactive oxygen species (ROS) generation in diverse cell types. It has demonstrated significant biological activity in preclinical studies, including induction of apoptosis in acute myeloid leukemia (AML) cell lines[1], and is able to inhibit platelet aggregation through mechanisms involving both NOX-dependent and NOX-independent pathways[3]. Mechanistically, VAS3947 alkylates cysteine thiols of glutathione and proteins, leading to protein aggregation, misfolding, and subsequent activation of the unfolded protein response (UPR) and endoplasmic reticulum (ER) stress pathways, ultimately causing apoptosis[1]. Additionally, VAS3947 does not interfere with xanthine oxidase, endothelial nitric oxide synthase (eNOS), or ROS detection assays[1][3].

Other names
VAS-3947VAS3947VAS 3947
02

Targets

NOX4 (NADPH oxidase 4)EIF2AK3 (Pkr-like endoplasmic reticulum kinase)GSH (Glutathione)

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