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Molecular Glues

Molecular glues are small molecules that bring two proteins into contact, often to trigger ubiquitination. Lenalidomide and pomalidomide bind cereblon, the substrate receptor of a cullin 4 ubiquitin ligase, and redirect it to new substrates. Cereblon was identified as a thalidomide-binding protein in 2010, and in 2014 lenalidomide was shown to drive degradation of the transcription factors Ikaros (IKZF1) and Aiolos (IKZF3). Mezigdomide is a further cereblon-binding degrader, while SJ3149 recruits casein kinase 1 alpha (CK1α) for degradation. Cyclosporin A follows a related principle, forming a complex with cyclophilin that was reported in 1991 to inhibit the phosphatase calcineurin. BI-3802 instead induces polymerization of its target protein, whereas bifunctional degraders sit in the sibling category PROTAC Degrader.

Cat. No.

A79511

CAS No.

3034876-85-9

VVD 065

VVD 065 is an allosteric modulator of the Keap1-Cul3 E3 ligase complex that functions as a molecular glue. By activating KEAP1, VVD 065 promotes the degradation of NRF2, an essential regulator of antioxidant defenses. This compound has demonstrated the ability to inhibit tumor growth in non-small cell lung cancer and esophageal squamous cell carcinoma xenograft models. VVD 065 serves as a valuable tool for research on cancer biology and therapeutic strategies targeting oxidative stress responses.

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5 mg

$690.00

10 mg

$1,135.00

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Molecular Glues

VVD 065