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Tocris Bioscience™ VVD 065
SDP

Catalog No. 88752 Shop All R&D Systems Products
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88-752 2 mg
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Catalog No. 88-752 Supplier Tocris Bioscience™ Supplier No. 8875/2
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Description

Covalent allosteric NRF2 inhibitor

VVD 065 is a NRF2 inhibitor acting via a covalent allosteric molecular glue mechanism. Through covalent engagement of C151 on KEAP1, VVD 065 promotes NRF2 degradation by enhancing formation of the KEAP1-CUL3 ubiquitin ligase complex. With potent target engagement (TE50 = 9 nm in KYSE70 cells) and selectivity over unrelated targets, VVD 065 inhibits NRF2-dependent cell growth. In vitro, VVD 065 inhibits NRF2 transcriptional activity and reduces the expression of NRF2 target genes. In vivo, VVD 065 induces tumor growth inhibition and downregulation of NRF2 signaling in cell-line and patient-derived mouse xenograft models, synergizing with other combinations. VVD 065 is orally bioavailable.

Specifications

Chemical Name or Material 1-[(3R)-3-[3-(4-Amino-1,3,5-triazin-2-yl)-5-chlorophenyl]-4-morpholinyl]-2-propen-1-one
CAS 3034876-85-9
Quantity 2 mg
Target Molecular Glues
Molecular Formula C16H16ClN5O2
Purity 98%
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