Leelamine | Intracellular cholesterol inihibitor

CAS:
16496-99-4
Catalog Number:
10-2955
Activity:
Intracellular cholesterol inhibitor
Chemical Name:
(1R,4aS,10aR)-1,2,3,4,4a,9,10,10a-Octahydro-1-,4a-dimethyl-7-(1-methylethyl)-1-phenanthrenemethanamine hydrochloride
Alternate Name:
Lylamine HCl; (+)-Dehydroabietylamine HCl
Molecular Weight:
321.93
Molecular Formula:
C20H31N•HCl
Solubility:
Soluble in DMSO (up to 40 mg/ml) or in Water (up to 9 mg/ml).
Physical Properties:
Off-white or beige solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
10 mg$50.00
50 mg$200.00

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

CAS:
16496-99-4
Catalog Number:
10-2955
Activity:
Intracellular cholesterol inhibitor
Chemical Name:
(1R,4aS,10aR)-1,2,3,4,4a,9,10,10a-Octahydro-1-,4a-dimethyl-7-(1-methylethyl)-1-phenanthrenemethanamine hydrochloride
Alternate Name:
Lylamine HCl; (+)-Dehydroabietylamine HCl
Molecular Weight:
321.93
Molecular Formula:
C20H31N•HCl
Solubility:
Soluble in DMSO (up to 40 mg/ml) or in Water (up to 9 mg/ml).
Physical Properties:
Off-white or beige solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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