Preferred Label : Trodusquemine;
NCIt synonyms : Cholestane-7,24-diol, 3-((3-((4-((3-aminopropyl)amino)butyl)amino)propyl)amino)-,
24-(Hydrogen Sulfate), (3beta,5alpha,7alpha,24R)-; (24R)-3beta-((3-((4-((3-aminopropyl)amino)butyl)amino)propyl)amino)-7alpha-hydroxy-5alpha-cholestan-24-yl
Hydrogen Sulfate;
NCIt definition : A naturally-occurring cholestane and non-competitive, allosteric inhibitor of protein
tyrosine phosphatase 1B (PTP1B), with potential hypoglycemic, anti-diabetic, anti-obesity,
and antineoplastic activities. Upon administration, trodusquemine selectively targets
and inhibits PTP1B, thereby preventing PTP1B-mediated signaling. This prevents the
dephosphorylation of the insulin receptor, which improves insulin signaling and insulin
sensitivity, and decreases blood glucose levels. In susceptible cancer cells, inhibition
of PTP1B causes a reduction of tumor cell proliferation. In addition, as trodusquemine
can cross the blood-brain barrier (BBB), it centrally suppresses appetite and causes
weight loss. PTP1B, a tyrosine phosphatase, is elevated in certain cancer cells; it
is specifically upregulated in human epidermal growth factor receptor 2 (HER2)-driven
cancers where it promotes cell growth, and is correlated with a poor prognosis and
increased metastatic potential. In diabetes, PTP1B upregulation plays a major role
in insulin resistance.;
UNII : KKC12PIF16;
InChIKey : WUJVPODXELZABP-FWJXURDUSA-N;
CAS number : 186139-09-3;
Molecule name : MSI-1436; MSI-1436C;
Origin ID : C123882;
UMLS CUI : C1869838;
Automatic exact mappings (from CISMeF team)
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
