Preferred Label : Rac/Cdc42 Inhibitor MBQ-167;
NCIt synonyms : Rac/Cdc-42 Inhibitor MBQ-167; Rac/Cdc42 Guanine Nucleotide Association Inhibitor MBQ-167; 9-Ethyl-3-(5-phenyl-1H-1,2,3-triazol-1-yl)-9H-carbazole;
NCIt related terms : MBQ-167;
NCIt definition : An orally bioavailable inhibitor of the Rho GTPases Ras-related C3 botulinum toxin
substrate (Rac) and cell division control protein 42 homolog (Cdc42), with potential
antineoplastic activity. Upon oral administration, Rac/Cdc42 inhibitor MBQ-167 targets,
binds to and inhibits the activity of the GTP-binding proteins Rac and Cdc42 that
are expressed on certain cancer cells and immunosuppressive immune cells in the tumor
microenvironment (TME). This inhibits p21-activated kinase (PAK) and signal transducer
and activator of transcription 3 (STAT3) signaling, induces cell-cycle arrest and
apoptosis, and inhibits cancer cell proliferation and migration. MBQ-167 also reduces
tumor-infiltrating macrophages and myeloid-derived suppressor cells (MDSCs) in the
TME, which may abrogate the immunosuppressive nature of the TME. Rac and Cdc42, overexpressed
or hyperactivated in various cancers, are homologous, small GTPases that regulate
epithelial to mesenchymal transition, cell migration, invasion, and cell cycle progression
and metastasis.;
UNII : RRY5XN588Q;
CAS number : 2097938-73-1;
Molecule name : MBQ-167; MBQ 167;
NCI Metathesaurus CUI : CL1921214;
Origin ID : C202250;
UMLS CUI : C5907970;
Semantic type(s)
- concept_is_in_subset
- has_target
