AR7 是一种非典型的RARA/RARα(视黄酸受体 α) 拮抗剂,能够特异性激活伴侣介导的自噬活性,对自噬无影响。
产品描述
AR7 is a retinoic acid receptor α (RARα) antagonist.
体外活性
Chaperone-mediated autophagy (CMA) contributes to cellular quality control and the cellular response to stress through the selective degradation of cytosolic proteins in lysosomes. Decrease in CMA activity occurs in aging and in age-related disorders. Signaling through the retinoic acid receptor alpha (RARα) inhibits CMA. AR7, an RARα antagonist, significantly activates CMA activity in mouse fibroblasts. A marked increase in CMA-activating potency is found when AR7 and GR1 are combined, supporting their cooperative effect. Treatment with the transcriptional repressor Actinomycin D partially reduces the stimulatory effect of AR7 on CMA, consistent with transcriptional changes contributing to the upregulation of CMA. The antagonistic effect of the retinoid derivatives likely results from a combination of tight binding to RARα and high stability.
Cas No.
80306-38-3
分子式
C15H12ClNO
分子量
257.72
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years