VAV1 degrader-3

SKU: orb2802569

Description

VAV1 degrader-3 is an orally bioavailable molecular glue that induces the degradation of VAV1. This action suppresses immune cell activation, proliferation, and cytokine release, making it a valuable research tool for investigating inflammatory and autoimmune disease mechanisms in both cellular and animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 3050683-38-7
• MW: 392.84
• Purity: >99.99% (May vary between batches)
• Formula: C₂₂H₁₇ClN₂O₃
• SMILES: O=C1C=CC=CN1C2=CC=C(C=C2)C=3C=CC=C(C3Cl)C4C(=O)NC(=O)CC4
• Target: Molecular Glues

Bioactivity

• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

VAV1degrader3, MRT-6160

Compound Identifiers

PubChem CID

171846794