Autophagy inhibitor
Hydroxychloroquine Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
Function: Autophagy inhibitor
Target: TLR9
Chemical name: 2-[[4-[(7-chloro-4-quinolinyl)amino]pentyl]ethylamino]-ethanol, sulfate (1:1)
Formula: C18H28ClN3O5S
Molecular weight: 433.95
Purity: 99.86% (HPLC)
Solubility: 87 mg/mL (water)
Size: 10 mg
Storage: 3 years -20°C powder, 2 years -80°C in solvent
Regulatory/ Restrictions: For laboratory use only.
In vitro: Hydroxychloroquine Sulfate is a potent inhibitor of autophagy. It prevents lysosomal acidification, thereby interfering with a key step in the autophagic process. HCQ treatment inhibits RCC (renal cell cancer) cell growth, promotes apoptosis, inhibits mitochondrial oxygen consumption, and increases rates of glycolysis[2].
In vivo: The treatment of Hydroxychloroquine Sulfate reduces the infarct size in an in vivo rat model of I/R injury and the cardioprotective effect of Hydroxychloroquine is ERK1/2 dependent[3]. In addition, Hydroxychloroquine Sulfate shows an early vascular protective effect. HCQ seems to prevent the occurrence of endothelial dysfunction(ED) in treated animals[4].
References:
[1] Ramser B, et al.J Invest Dermatol, 2009,129(10):2419-26.
[2] Lee HO, et al. PLoS One. 2015, 10(7): e0131464.
[3] Bourke L, et al. PLoS One. 2015, 10(12):e0143771.
[4] Marta Mosca, et al. 2013 ACR/ARHP Annual Meeting.