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NSCA-1

Development stage: Preclinical
Modality: Small Molecules

Overview

NSCA-1 is a novel N-substituted coumalamide derivative, belonging to the 2-pyrone class of compounds. It has been investigated for its potential to overcome multidrug resistance in hepatocellular carcinoma, specifically by sensitizing HepG2/ADR cells to the chemotherapeutic agent Adriamycin (doxorubicin). The drug's mechanism of action involves the inhibition of Akt kinase activity and the reduction of Akt phosphorylation at Ser473, which leads to decreased phosphorylation of GSK-3β. Additionally, NSCA-1 has been shown to boost the intracellular accumulation of Adriamycin by reducing the expression of P-glycoprotein (P-gp) and to enhance cell apoptosis through the p53-dependent apoptotic pathway.

Other names: N-substituted coumalamide derivative-1

Targets

ABCB1 (P-glycoprotein)TP53 (Cellular Tumor Antigen p53 R175H)AKT (RAC-alpha serine/threonine-protein kinase)

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