1446-61-3
Chemical Structure
Leelamine
- CAS 番号: 1446-61-3
- Formula:C20H31N
- Molecular Weight:285.48
IUPAC Name: ((1R,4aS,10aR)-7-isopropyl-1,4a-dimethyl-1,2,3,4,4a,9,10,10a-octahydrophenanthren-1-yl)methanamine
InChIKey: JVVXZOOGOGPDRZ-SLFFLAALSA-N
SMILES: NC[C@]1(C)CCC[C@]2(C)C3=C(CC[C@@]12[H])C=C(C(C)C)C=C3
Biological Activity: Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC50 value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells[1][2][3].
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Leelamine | 95.69% | Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC50 value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells. | ||||||||||||||||||||
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- [1]. Merarchi M, et, al. A Brief Overview of the Antitumoral Actions of Leelamine. Biomedicines. 2019 Jul 19;7(3):53. [Content Brief]
- [2]. Kuzu OF, Gowda R, Sharma A, Robertson GP. Leelamine mediates cancer cell death through inhibition of intracellular cholesterol transport. Mol Cancer Ther. 2014;13(7):1690-1703. [Content Brief]
- [3]. Aicher TD, et al. Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK). Bioorg Med Chem Lett. 1999 Aug 2;9(15):2223-8. [Content Brief]
Keywords
