| Description | AR7 is a retinoic acid receptor α (RARα) antagonist. |
| In vitro | 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. |
| molecular weight | 257.71 |
| Molecular formula | C15H12ClNO |
| CAS | 80306-38-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 5.5 mg/mL (21.34 mM), Sonication is recommended. |
| References | 1. Anguiano J, et al. Chemical modulation of chaperone-mediated autophagy by retinoic acid derivatives. Nat Chem Biol. 2013 Jun;9(6):374-82. 2. Jiang S, Wang X, He Y, et al. Suppression of USP7 induces BCR-ABL degradation and chronic myelogenous leukemia cell apoptosis[J]. Cell Death & Disease. 2021, 12(5): 1-12. |
| Citations | 1. Jiang S, Wang X, He Y, et al. Suppression of USP7 induces BCR-ABL degradation and chronic myelogenous leukemia cell apoptosis. Cell Death & Disease. 2021, 12(5): 1-12. 2. Xiong Q, Sun H, Xing W, et al.WDR45 mutation dysregulates iron homeostasis by promoting the chaperone-mediated autophagic degradation of ferritin heavy chain in an ER stress/p38 dependent mechanism.Free Radical Biology and Medicine.2023 3. Xiong Q, Sun H, Wang Y, et al.Lipid droplet accumulation in Wdr45-deficient cells caused by impairment of chaperone-mediated autophagic degradation of Fasn.Lipids in Health and Disease.2024, 23(1): 91. |