3034876-85-9
Chemical Structure
VVD 065
- CAS No.: 3034876-85-9
- Formula:C16H16ClN5O2
- Molecular Weight:345.78
IUPAC Name: (R)-1-(3-(3-(4-amino-1,3,5-triazin-2-yl)-5-chlorophenyl)morpholino)prop-2-en-1-one
InChIKey: BMXYLROANWRSJZ-ZDUSSCGKSA-N
SMILES: C=CC(N1[C@H](C2=CC(C3=NC=NC(N)=N3)=CC(Cl)=C2)COCC1)=O
Biological Activity: VVD 065 is an orally active KEAP1-dependent NRF2 molecular glue degrader with a KEAP1 KD of 65 nM. VVD 065 covalently engages KEAP1 at Cys151, allosterically stabilizes KEAP1-CUL3 complex formation and enhances NRF2 polyubiquitination and proteasomal degradation. VVD 065 can be used for the research of esophageal squamous cell carcinoma, lung cancer, head-and-neck cancer, uterine cancers[1][2][3].
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VVD 065 | 99.71% | VVD 065 is an orally active KEAP1-dependent NRF2 molecular glue degrader with a KEAP1 KD of 65 nM. VVD 065 covalently engages KEAP1 at Cys151, allosterically stabilizes KEAP1-CUL3 complex formation and enhances NRF2 polyubiquitination and proteasomal degradation. VVD 065 can be used for the research of esophageal squamous cell carcinoma, lung cancer, head-and-neck cancer, uterine cancers. | ||||||||||||||||||||
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References
- [1]. Adamopoulos C, et al. Turning KEAP1 against NRF2. Nat Chem Biol. 2026 May;22(5):680-682. [Content Brief]
- [2]. Roy N, et al. Abstract PR011: Discovery of VVD-065, a first-in class allosteric molecular glue of the Keap1-Cul3 E3-ligase complex for the treatment of NRF2 activated cancers. Mol Cncer Ther. 2023 Dec 01;22:PR011.
- [3]. Roy N, et al. A Covalent Allosteric Molecular Glue Suppresses NRF2-Dependent Cancer Growth. Cancer Discov. 2026 May 1;16(5):953-975. [Content Brief]
