Preferred Label : ENPP1 Inhibitor RBS2418;
NCIt definition : A selective small molecule inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase
1 (ENPP1), with potential immunomodulating and antineoplastic activities. Upon administration,
ENPP1 inhibitor RBS2418 targets and binds to ENPP1, thereby inhibiting the activity
of ENPP1. This inhibits ENPP1-mediated 2'-3'-cyclic guanosine monophosphate-adenosine
monophosphate (cGAMP) and adenosine triphosphate (ATP) hydrolysis and stabilizes extracellular
endogenous cGAMP and ATP. This leads to the extracellular accumulation of cGAMP and
ATP, and inhibits the production of immunosuppressive adenosine in the tumor microenvironment
(TME). This allows for induction of anticancer immune responses. ENPP1, overexpressed
in a number of tumor types, mediates nucleotide recycling by breaking down ATP to
AMP, which is then converted to adenosine. It suppresses anti-tumor immune responses
and increases metastasis.;
Molecule name : RBS-2418; RBS 2418;
NCI Metathesaurus CUI : CL1792003;
Origin ID : C187127;
UMLS CUI : C5706374;
Semantic type(s)
- concept_is_in_subset
- has_target
