Drug intelligence / Profile preview

NSC126405

Development stage
Preclinical
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
Oral
01

Overview

NSC126405 is a small-molecule inhibitor of the interaction between DEP domain-containing mTOR-interacting protein (DEPTOR) and the mechanistic target of rapamycin (mTOR). By binding specifically to DEPTOR, NSC126405 prevents DEPTOR from binding to mTOR, thereby disrupting the inhibitory effect of DEPTOR on mTOR complexes (mTORC1 and mTORC2). This disruption leads to the activation of mTORC1 and mTORC2 signaling pathways. In multiple myeloma cells, which often overexpress DEPTOR, treatment with NSC126405 induces cell cycle arrest, inhibits autophagy, and triggers apoptosis, demonstrating potent in vitro and in vivo cytotoxicity. It has also been studied in breast cancer models to reverse the effects of DEPTOR overexpression.

Other names
(2,3,4,5-tetrachlorocyclopenta-2,4-dien-1-ylidene)hydrazine
02

Targets

mTOR (Mammalian target of rapamycin kinase)DEPTOR

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