VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors[1][2][3][4].
Molecular Weight:
344.80
Purity:
99.91
CAS Number:
[3034880-93-5]
Formula:
C17H17ClN4O2
Target:
Keap1-Nrf2,Molecular Glues
Application Notes:
MCE Product type: Reference compound1
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