product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
VVD 065
catalog :
8875/2
quantity :
2 mg
price :
259 USD
more info or order :
Tocris Bioscience product webpage
product information
brand :
Tocris
catalog number base :
8875
SKU :
8875/2
product name :
VVD 065
units size :
2 mg
description :
Covalent allosteric NRF2 inhibitor
target :
Molecular Glues
category :
Small Molecules
purity :
98%
observed molecular weight :
345.79
url print :
?utm_source=biocompare&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
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.
top caption :
Covalent allosteric NRF2 inhibitor
extended description :
Covalent allosteric NRF2 inhibitor
chemical name text :
1-[(3R)-3-[3-(4-Amino-1,3,5-triazin-2-yl)-5-chlorophenyl]-4-morpholinyl]-2-propen-1-one
formula :
C16H16ClN5O2
formula text :
C16H16ClN5O2
cas num :
3034876-85-9
USD :
259 USD
product details :
Covalent allosteric NRF2 inhibitor
storage :
Store at -20°C
more info or order :
Tocris Bioscience product webpage
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK