Hydroxychloroquine sulfate (747-36-4) is a lysosomotropic agent which inhibits autophagy and triggers apoptosis in a variety of cell types.1,2 Augments the anticancer activity of DNA-damaging chemotherapy.3 Antiinflammatory activity. Decreases cell surface expression of TNFα receptors in U937 cells.4 Hydroxychloroquine sulfate has been used to treat alopecia successfully5 and is a clinically useful antimalaria agent. Cell permeable and active in vivo.
1) Boya et al. (2005), Inhibition of macroautophagy triggers apoptosis; Mol. Cell Biol., 25 1025
2) Xie et al. (2013), Coordinate autophagy and mTOR pathway inhibition enhances cell death in melanoma; PLoS One, 8 e55096
3) Pan et al. (2011), Targeting autophagy augments in vitro and in vivo antimyeloma activity of DNA-damaging chemotherapy; Clin. Cancer Res., 150 3248
4) Jeong et al. (2002), Chloroquine decreases cell-surface expression of tumor necrosis factor receptors in human histiocytic U-937 cells; Immunology, 105 83
5) Stephan et al. (2013), Successful treatment of alopecia totalis wih hydroxychloroquine: report of 2 cases; J. Am. Acad. Dermatol., 68 1048