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
Dehydroabiethylamine is a primary amine with high molecular weight; shows a strong antibiotic effect with a broad spectrum of activity against Staphylococcus p.a. (sic), Escherichia coli, Mycobacterium tuberculosis, and Candida albicans.
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
