Leelamine HCl (16496-99-4) is a lysosomotropic, intracellular cholesterol transport inhibitor with potential chemotherapeutic activity. Induces cholesterol accumulation in lysosomal/endosomal cell compartments via inhibition of autophagic flux.¹ Induces apoptosis in breast cancer², melanoma³ and prostate cancer cells⁴. A selective inducer of cytochrome P450 2B.⁵ Inhibits pyruvate dehydrogenase kinase (PDK), IC₅₀=9.5 µM.⁶

References/Citations
1) Kuzu et al. (2014), Leelamine mediated cancer cell death through inhibition of intracellular cholesterol transport; Mol. Cancer Ther., 13 1690
2) Sehrawat et al. (2017), Cancer-selective death of human breast cancer cells by leelamine is mediated by bax and bak activation; Am. Mol. Carcinolg., 56 337
3) Chen et al. (2017), Targeting cholesterol transport in circulating melanoma cells to inhibit metastasis; Pigment Cell Melanoma Res., 30 541
4) Singh et al. (2018), Therapeutic Potential of Leelamine, a Novel Inhibitor of Androgen Receptor and Castration-Resistant Prostate Cancer; Mol. Cancer Ther., 17 2079
5) Sim et al. (2015), Selective induction of hepatic cytochrome P450 2B activity by leelamine in vivo, as a potent novel inducer; Arch. Pharm. Res., 38 725
6) Aicher et al. (1999), Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK); Bioorg. Med. Chem. Lett., 9 2223