Piperlongumine - Piplartine

Based on 230 publications in PubMed 9 10 230

Axon 2488

CAS [20069-09-4]

MF C17H19NO5
MW 317.34

Purity: 99%
Soluble in DMSO

Piperlongumine

Description

Natural alkaloid with potent cytotoxic activity which has been related to an increased reactive oxygen species (ROS) generation in cancer cells (through direct GSTP1 interaction), down-regulation of nuclear factor-kB (NF-kB) activation and induction of rapid depletion of the androgen receptor (AR) in prostate cancer cells. Moreover, Piperlongumine (or Piplartine) was found to induce apoptosis and autophagy through modulation of the PI3K/Akt/mTOR pathway in human lung cancer cells, and potently inhibited ligand-stimulated STAT3 nuclear translocation.

R.C. Barcelos et al. Design and synthesis of N-acylated aza-goniothalamin derivatives and evaluation of their in vitro and in vivo antitumor activity. ChemMedChem. 2014 Dec;9(12):2725-43.

F. Wang et al. Piperlongumine induces apoptosis and autophagy in human lung cancer cells through inhibition of PI3K/Akt/mTOR pathway. Int J Immunopathol Pharmacol. 2015 Sep;28(3):362-73.

S. Ginzburg et al. Piperlongumine inhibits NF-κB activity and attenuates aggressive growth characteristics of prostate cancer cells. Prostate. 2014 Feb;74(2):177-86.

U. Bharadwaj et al. Drug-repositioning screening identified piperlongumine as a direct STAT3 inhibitor with potent activity against breast cancer. Oncogene. 2015 Mar 12;34(11):1341-53.

D.J. Adams et al. Synthesis, cellular evaluation, and mechanism of action of piperlongumine analogs. Proc Natl Acad Sci U S A. 2012 Sep 18;109(38):15115-20.

M. Jarvius et al. Piperlongumine induces inhibition of the ubiquitin-proteasome system in cancer cells. Biochem Biophys Res Commun. 2013 Feb 8;431(2):117-23.

Apoptosis Cell Signaling & Oncology Miscellaneous Pain & Inflammation Transcription Factors p53-Tumor Suppression NF-κB JAK-STAT PI3K-Akt-mTOR DNA-damage Response Ubiquitin STAT3 GSTP EC 2.5.1.18

Natural alkaloid with potent cytotoxic activity

Chemical name

(E)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one

Parent CAS No.

[20069-09-4]

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