VAV1 Degrader

MRT-6160 (Example 185) is an orally active VAV1 molecular glue degrader (DC₅₀: 7 nM). MRT-6160 reduces immune cell activation, immune cell proliferation and the production of various cytokines. MRT-6160 can be used for research of inflammatory or autoimmune disorder. MRT-6160 inhibits disease progression in experimntal autoimmune encephalomyelitis (EAE) mouse model, Collagen-induced arthritis (CIA) mouse model, etc..

VAV1 degrader-2 is a molecular glue degrader based on targeting Vav guanine nucleotide exchange factor 1 (VAV 1) with a DC₅₀ of 4.41 nM. VAV1 degrader-2 can be used in the study of inflammatory and autoimmune diseases.

MRT-23227 is a CRBN-recruiting molecular glue degrader targeting VAV1. MRT-23227 binds to the tryptophan triad pocket of CRBN, forms a ternary complex with the SH3c domain of VAV1, and induces proteasomal degradation of VAV1 through hydrogen-bond interactions between CRBN residues and the RT loop and side chains of VAV1. MRT-23227 can be used in the research of T-cell leukemia and lymphoma.

(R)-MRT-6160 is a molecular glue degrader targeting VAV1, with a DC₅₀ of 40.93 nM. (R)-MRT-6160 induces VAV1 ubiquitination and proteasomal degradation by forming a CRBN-(R)-MRT-6160-VAV1 ternary complex, thereby inhibiting signaling downstream of the T/B cell receptor. (R)-MRT-6160 can be used in leukemia-related research.

VAV1 degrader-4 is a VAV1 molecular glue degrader with a DC₅₀ value of 3.93 nM for VAV1 in Jurkat cells. VAV1 degrader-4 can dose-dependently inhibit the production of IL-2. VAV1 degrader-4 can be used for research on autoimmune diseases.

(S)-VAV1 degrader-1 is a VAV1 molecular glue degrader with DC₅₀ = 3.07 nM. (S)-VAV1 degrader-1 is used for research on VAV1-related diseases, such as inflammation and immune-related diseases.