Leelamine

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].

Product Specifications

CAS Number

[1446-61-3]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Cannabinoid Receptor; PDK-1

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/leelamine.html

Concentration

10mM

Purity

98.36

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

NC[C@]1(C)CCC[C@]2(C)C3=C(CC[C@@]12[H])C=C(C(C)C)C=C3

Molecular Formula

C20H31N

Molecular Weight

285.48

Precautions

H315, H319, H335

References & Citations

[1]Merarchi M, et, al. A Brief Overview of the Antitumoral Actions of Leelamine. Biomedicines. 2019 Jul 19;7 (3) :53. |[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. |[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.