产品名称
K67, ≥98% (HPLC)
InChI key
VUIVGOOWLHGDPZ-UHFFFAOYSA-N
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
Quality Level
相关类别
Biochem/physiol Actions
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。
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)。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_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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