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VAV1 degrader-3 is a molecular gel degrader targeting VAV1 with a DC50 of 7 nM. VAV1 is a key signaling protein downstream of T cell and B cell receptors. VAV1 degrades VAV1 to degrader-3, which significantly reduces the level of cytokines associated with immune-mediated diseases, but has no effect on other proteins, and can be used to study inflammatory or autoimmune diseases.In mouse models of various diseases, such as experimental autoimmune encephalomyelitis (EAE), colitis, and collagen-induced arthritis (CIA), VAV1 degraders the progression of disease.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $340 | Backorder | |
5 mg | $970 | Backorder | |
25 mg | $1,520 | Backorder | |
50 mg | $1,980 | Backorder |
Description | VAV1 degrader-3 is a molecular gel degrader targeting VAV1 with a DC50 of 7 nM. VAV1 is a key signaling protein downstream of T cell and B cell receptors. VAV1 degrades VAV1 to degrader-3, which significantly reduces the level of cytokines associated with immune-mediated diseases, but has no effect on other proteins, and can be used to study inflammatory or autoimmune diseases.In mouse models of various diseases, such as experimental autoimmune encephalomyelitis (EAE), colitis, and collagen-induced arthritis (CIA), VAV1 degraders the progression of disease. |
In vitro | VAV1 degrader-3 (0-1μM, 24h) induces VAV1 degradation, thereby reducing CD69 expression mediated by the B cell receptor and the secretion of IL-6 and IgG in primary human B cells.
VAV1 degrader-3 inhibits the growth of B lymphoma cells in a concentration-dependent manner. [1] |
In vivo | VAV1 degrader-3 (1-10 mg/kg, oral) inhibits the progression of experimental autoimmune encephalomyelitis (EAE) in the EAE mouse model in a dose-dependent manner.
In the T cell transfer-induced colitis model, VAV1 degrader-3 (1 mg/kg, oral) inhibited colitis. In the collagen-induced arthritis model, VAV1 degrader-3 (1 mg/kg, 21 days, oral) reduced the production of anti-collagen II IgG1 antibodies and prevented the progression of arthritis. [1] |
Molecular Weight | 392.83 |
Formula | C22H17ClN2O3 |
Cas No. | 3050683-38-7 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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