Lycorine 

Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. Lycorine is a potent and orally active SCAP inhibitor with a K_d value 15.24 nM. Lycorine downregulates the SCAP protein level without changing its transcription^[2]. Lycorine is also a melanoma vasculogenic inhibitor^[3]. Lycorine can be used for the study of prostate cancer and metabolic diseases^[2].

Kd: 15.24 nM (SCAP)^[1]

Lycorine inhibits cell proliferation in a dose-dependent manner in the abovementioned 4 PCa cell lines, and the IC₅₀ ranged from 5 μM to 10 μM., it also shows Lycorine has little effects on PNT1A cell's proliferation^[1].
SCAP (SREBF chaperone) is an ER-toGolgi transport protein, undergoes a conformational change, and regulates/preserves SREBFs in the ER by forming a complex with INSIG1 (insulin induced gene 1)^[2].
Lycorine (5-40 μM; 16 hours) significantly suppresses SREBFs activity (up to -70%) in a dosedependent manner and does not cause obvious cytotoxicity in cells^[2].
Lycorine (10-20 μM; 2-16 hours) dose- and time-dependently decreases the mature SREBF1 and SREBF2 proteins in HL-7702 cells^[2].
Lycorine (20 μM; 16 hours) neither activates NR1H3 transcription nor affect NR1H3 target genes, including ABCG5? and ABCG8, but Sterols activates NR1H3 transcription activity^[1].
Lycorine (0-25 μM; 48 hours) treatment markedly suppresses the expression of vascular endothelial (VE)-cadherin in a dose-dependent manner and also slightly diminishes the expression of Sema4D in C8161 cells. However, the expression of the other six genes is not affected^[3].
Lycorine (0-25 μM; 48 hours) treatment markedly reduces VE-cadherin protein levels in C8161 cells in a dose-dependent fashion^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lycorine (oral chow; 15 mg/kg, 30 mg/kg; once daily) alleviates fat accumulation and metabolic syndrome, increases lipolysis and betaoxidation of fatty acid along with precursor and mature SREBFs in mice ^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

287.31

C₁₆H₁₇NO₄

476-28-8

Solid

White to off-white

O[C@@H]1[C@@H](O)C=C(CC2)[C@@]3([H])N2CC4=C([C@@]31[H])C=C(OCO5)C5=C4

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Hu M, et al.Lycorine is a novel inhibitor of the growth and metastasis of hormone-refractory prostate cancer.Oncotarget. 2015 Jun 20;6(17):15348-61.

  [2]. Zu-Guo Zheng, et al. Discovery of a Potent SCAP Degrader That Ameliorates HFD-induced Obesity, Hyperlipidemia and Insulin Resistance via an Autophagy-Independent Lysosomal Pathway. Autophagy. 2020 May 20;1-22.  [Content Brief]

  [3]. [1].Liu, R. et al. Lycorine hydrochloride inhibits metastatic melanoma cell-dominant vasculogenic mimicry. Pigment cell & melanoma research 25, 630-638, doi:10.1111/j.1755-148X.2012.01036.x (2012).  [Content Brief]