质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 10 mg/mL, clear
储存温度
2-8°C
SMILES字符串
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
生化/生理作用
K67是一种特异性抑制剂，可抑制p62/SQSTM1的KEAP1（Kelch样环氧氯丙烷相关蛋白-1）DC（双甘氨酸重复区和C端区域）结构域与S349磷酸化（人Ser349，小鼠Ser351）KIR（Keap1相互作用区域）之间的相互作用，从而防止磷酸化p62阻断KEAP1-DC和NRF2（核因子红细胞2相关因子2）DLGex基序结合。K67通过恢复KEAP1驱动的NRF2泛素化和降解，能够有效抑制高细胞p62 S351磷酸化的HCC（肝细胞癌）培养物的增殖（使用50 μM K67处理72小时后，抑制了59％Huh7细胞增殖）。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Daisuke Yasuda et al.
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
Tetsuya Saito et al.
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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