All Photos(1)
2-Acetonyl-1,4-bis[(4-ethoxybenzensulfonyl)amino]naphthalene, N,N′-(2-(2-Oxopropyl)naphthalene-1,4-diyl)bis(4-ethoxybenzenesulfonamide), N-[2-Acetonyl-4-(4-ethoxybenzenesulfonylamino)naphthalene-1-yl]-4-ethoxybenzenesulfonamide
C29H30N2O7S2
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Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
SMILES string
CC(CC1=C(NS(C2=CC=C(OCC)C=C2)(=O)=O)C3=C(C=CC=C3)C(NS(C4=CC=C(OCC)C=C4)(=O)=O)=C1)=O
Biochem/physiol Actions
K67 is a specific inhibitor against the interaction between KEAP1 (Kelch-like ECH-associated protein 1) DC (double glycine repeat and C-terminal region) domain and S349-phosphorylated (human Ser349, mouse Ser351) KIR (Keap1-interacting region) of p62/SQSTM1, thereby preventing phospho-p62 from blocking KEAP1-DC and NRF2 (nuclear factor erythroid 2-related factor 2) DLGex motif association. K67 effectively inhibits the proliferation of HCC (hepatocellular carcinoma) cultures (by 59% of Huh7 cells post 72 h 50 μM K67 treatment) with high cellular p62 S351-phosphorylation by restoring KEAP1-driven NRF2 ubiquitination and degradation.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Bioorganic & medicinal chemistry letters, 26(24), 5956-5959 (2016-11-15)
The Keap1-Nrf2 system is involved not only in biological defense but also in malignancy progression and chemoresistance. The ubiquitin-binding protein p62/Sqstm1 (p62), which is highly expressed in several cancers, competes with Nrf2 for Keap1 binding, leading to activation of Nrf2-mediated
Nature communications, 7, 12030-12030 (2016-06-28)
p62/Sqstm1 is a multifunctional protein involved in cell survival, growth and death, that is degraded by autophagy. Amplification of the p62/Sqstm1 gene, and aberrant accumulation and phosphorylation of p62/Sqstm1, have been implicated in tumour development. Herein, we reveal the molecular
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