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VVD 065 is an NRF2 inhibitor that functions through a covalent allosteric binding mechanism. It promotes the degradation of NRF2 by covalently bonding with C151 on KEAP1, thereby enhancing the formation of the KEAP1-CUL3 ubiquitin ligase complex. With potent target binding affinity (TE50 of 9 nM in KYSE70 cells) and selectivity for unrelated targets, VVD 065 effectively inhibits NRF2-associated cell growth.
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | VVD 065 is an NRF2 inhibitor that functions through a covalent allosteric binding mechanism. It promotes the degradation of NRF2 by covalently bonding with C151 on KEAP1, thereby enhancing the formation of the KEAP1-CUL3 ubiquitin ligase complex. With potent target binding affinity (TE50 of 9 nM in KYSE70 cells) and selectivity for unrelated targets, VVD 065 effectively inhibits NRF2-associated cell growth. |
| In vitro | VVD 065 inhibits NRF2 transcriptional activity and reduces the expression of NRF2 target genes. |
| In vivo | VVD 065 promotes tumor growth inhibition and downregulates the NRF2 signaling pathway in both cell lines and mouse xenograft models, acting synergistically with other combinations. Additionally, VVD 065 is orally bioavailable. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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