Biological Activity:

AR7 is a specific and potent RARα antagonist (IC₅₀ < 100 nM) to stimulate Chaperone-mediated autophagy (CMA).It is a synthetic derivative of all-trans-retinoic acid developed through the structure-based chemical design. CMA contributes to cellular quality control and the cellular response to stress through the selective degradation of cytosolic proteins in lysosomes. A decrease in CMA activity occurs in aging and in age-related disorders (for example, neurodegenerative diseases and diabetes). AR7 working as a chemical enhancement of CMA protects cells from oxidative stress and from proteotoxicity, and supports a potential therapeutic opportunity when reduced CMA contributes to cellular dysfunction and disease. AR7 is the first chemical compound that affects CMA has the selectivity for this pathway without affecting macroautophagy.

How to Use:

In vitro:  AR7 was suggested to be used at 5-20 µM final concentration in vitro and in cellular assays.

In vivo:  n/a

Reference:

1. 1. Anguiano J, et al. Chemical modulation of chaperone-mediated autophagy by retinoic acid derivatives. (2013) Nat Chem Biol. 9(6):374-82.

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