VAV1 degrader-3

VAV1 degrader-3 (Example 185) is an orally active VAV1 molecular glue degrader (DC₅₀: 7 nM). VAV1 degrader-3 reduces immune cell activation, immune cell proliferation and the production of various cytokines. VAV1 degrader-3 can be used for research of inflammatory or autoimmune disorder. VAV1 degrader-3 inhibits disease progression in experimntal autoimmune encephalomyelitis (EAE) mouse model, Collagen-induced arthritis (CIA) mouse model, etc.^[1]. In Vitro: VAV1 degrader-3 (0-1 μM, 24 h) inhibtis B cell receptor-mediated activity, specifically, VAV1 degrader-3 inhibits CD69 expression, and IL-6, lgG secretion in PBMC cells isolated from human blood leukopaks^[1].
VAV1 degrader-3 (0-1 μM, 24 h) inhibits T cell receptor-mediated CD69 activation, IL-2 secretion, and proliferation of Primary T-cells^[1].
In Vivo: VAV1 degrader-3 (1-15 mg/kg, p.o.) inhibits disease progression in MOGss-ss-induced multiple sclerosis experimntal autoimmune encephalomyelitis (EAE) mouse model^[1].
VAV1 degrader-3 (1 mg/kg, p.o.) inhibits disease progression and reduces expression of calprotectin subunits (S100a8/S100a9) within colon tissue in a T cell transfer-induced model of colitis^[1].
VAV1 degrader-3 (1 mg/kg, p.o.) also inhibits disease progression collagen-induced arthritis (CIA) mouse model^[1].