Drug intelligence / Profile preview

N1,N11-diethylnorspermine

Development stage
Preclinical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
01

Overview

N1,N11-diethylnorspermine (DENSPM) is a synthetic polyamine analog and potent anticancer agent. It acts primarily by disrupting polyamine homeostasis in cells, modulating the activities of key biosynthetic enzymes such as ornithine decarboxylase (ODC) and S-adenosylmethionine decarboxylase (AdoMetDC). DENSPM induces the catabolic enzyme spermidine/spermine N1-acetyltransferase 1 (SSAT), leading to depletion of intracellular polyamines, which are essential for DNA structure, cell division, differentiation, and membrane function. This disruption can result in inhibition of tumor cell growth and proliferation. Preclinical studies have shown activity against various cancers including renal cell carcinoma, pancreatic cancer, melanoma, and lung cancer[4][7]. At low concentrations it may mimic endogenous polyamines in resistant cells; at higher concentrations it inhibits growth across multiple lines[7]. The compound is under investigation as a novel chemotherapeutic agent.

Other names
N(1),N(11)-diethylnorspermineDiethylnorspermineN1,N11-bis(ethyl)norspermine121749-39-1
02

Targets

ODC1 (Ornithine decarboxylase)AMD1 (S-adenosylmethionine decarboxylase)SAT1 (Spermidine/spermine N1-acetyltransferase 1)

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