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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

392.83

C₂₂H₁₇ClN₂O₃

3050683-38-7

ClC1=C(C2CCC(NC2=O)=O)C=CC=C1C3=CC=C(N4C(C=CC=C4)=O)C=C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Laura Ann Mcallister, et al. Targeted degradation of vav1. Patent. WO2024151547A1.