Drug intelligence / Profile preview

NISC-6

Development stage
Preclinical
Lead developer
The Pennsylvania State University
Modality
Small Molecules
01

Overview

NISC-6 is a naphthalimide-based isoselenocyanate (ISC) analog developed as a potential anti-tumor agent, specifically for the treatment of melanoma. It was designed to act as a dual inhibitor of DNA topoisomerase II and the PI3K/Akt signaling pathway. The incorporation of the isoselenocyanate group was intended to reduce the systemic and central nervous system toxicities associated with parent naphthalimide derivatives like mitonafide while simultaneously targeting the Akt3 pathway, which is frequently activated in sporadic melanomas. In preclinical studies, NISC-6 demonstrated inhibitory activity against topoisomerase II and reduced levels of Akt pathway proteins in human melanoma cells, although it was generally found to be less potent than its isothiocyanate counterpart, NITC-6.

02

Targets

AKT2 (Rac-beta serine/threonine-protein kinase)DNAAKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)TOP2A (DNA topoisomerase II)

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