Preferred Label : CXCR1/2 Inhibitor SX-682;
NCIt synonyms : (2-(((5-((4-Fluorophenyl)carbamoyl)pyrimidin-2-yl)thio)methyl)-4-(trifluoromethoxy)phenyl)boronic
Acid;
NCIt related terms : SX-682;
NCIt definition : An orally bioavailable, selective and reversible antagonist of C-X-C motif chemokine
receptors 1 (CXCR1) and 2 (CXCR2), with potential anti-inflammatory and antineoplastic
activities. Upon administration CXCR1/2 inhibitor SX-682 selectively and allosterically
binds to CXCR 1 and 2 and inhibits their activation by tumor-secreted chemokines.
This inhibits CXCR1/2-mediated signaling, reduces both recruitment and migration of
immunosuppressive myeloid-derived suppressor cells (MDSCs) and neutrophils in the
tumor microenvironment (TME), inhibits inflammatory processes and abrogates the immunosuppressive-induced
nature of the TME. This allows effector cells, such as natural killer (NK) cells and
cytotoxic T-lymphocytes (CTLs), to kill and eliminate cancer cells. This inhibits
tumor cell migration, metastasis, angiogenesis and tumor cell proliferation. CXCR1
and 2, G protein-coupled receptor proteins located on myeloid cells and certain tumor
cells, play key roles in the immunosuppressive nature of the TME, tumor metastasis,
therapy-resistance and myeloid cell suppression. They play a key role in inflammation
and their expression is elevated in several inflammatory-driven diseases.;
UNII : H5212R2DPM;
CAS number : 1648843-04-2;
Molecule name : SX 682; SX-682;
NCI Metathesaurus CUI : CL552163;
Origin ID : C150389;
UMLS CUI : C4725695;
Semantic type(s)
- concept_is_in_subset
