Piperlongumine

Catalog No.S7551 Synonyms: PPLGM, Piplartine

For research use only.

Piperlongumine (PPLGM, Piplartine), a natural alkaloid from Piper longum L., increases the level of reactive oxygen species (ROS) and selectively kills cancer cells. It is a direct TrxR1 inhibitor with suppressive activity against gastric cancer and a novel inhibitor of CRM1; also an inhibitor of PI3K/Akt/mTOR in human breast cancer cells.

Piperlongumine Chemical Structure

CAS No. 20069-09-4

Selleck's Piperlongumine has been cited by 20 publications

Purity & Quality Control

Choose Selective ROS Inhibitors

Biological Activity

Description Piperlongumine (PPLGM, Piplartine), a natural alkaloid from Piper longum L., increases the level of reactive oxygen species (ROS) and selectively kills cancer cells. It is a direct TrxR1 inhibitor with suppressive activity against gastric cancer and a novel inhibitor of CRM1; also an inhibitor of PI3K/Akt/mTOR in human breast cancer cells.
Targets
reactive oxygen species (ROS) [1] TrxR1 [5] CRM1 [6] PI3K/Akt/mTOR [7]
In vitro

Piperlongumine is a known ROS inducer which could induce pancreatic cancer cell death in cell culture[1] As a thromboxane A(2) receptor antagonist, Piperlongumine inhibits platelet aggregation. [2] Piperlongumine also promotes autophagy via inhibition of Akt/mTOR signalling and mediates cancer cell death. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ZR75-30 M2nHVmN6fG:2b4jpZ4l1gSCjc4PhfS=> NWLmWoJ{PzJiaILz Mmn5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gXnI4PS1|MDDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvQDcQvF2= M1rOUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUO3NVg3Lz5{NEmzO|E5PjxxYU6=
HCT116 MmGwR5l1d3SxeHnjbZR6KGG|c3H5 NHraNFU4OiCqcoO= MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME22MlA1|ryP NVPiZYxvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5N|cyQDZpPkK0PVM4OTh4PD;hQi=>
MDA-MB-231 NEnyVJVEgXSxdH;4bYNqfHliYYPzZZk> NX70TYtxPzJiaILz MmTuR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRThwNEdOwG0> MkntQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7M{exPFYoRjJ2OUO3NVg3RC:jPh?=
A549 M4PSemN6fG:2b4jpZ4l1gSCjc4PhfS=> NULheWtLPzJiaILz MmDlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUKyMlg2|ryP MkPvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7M{exPFYoRjJ2OUO3NVg3RC:jPh?=
WI38 NV;5cZVtS3m2b4TvfIlkcXS7IHHzd4F6 NV[2dJAzPzJiaILz NH\BNYREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBYUTN6IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NlYvPzkQvF2= NWnxfWt2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5N|cyQDZpPkK0PVM4OTh4PD;hQi=>
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PANC1 M3\MNGN6fG:2b4jpZ4l1gSCjc4PhfS=> M{T1XVI1KGi{cx?= MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQRW5EOSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhOjRiaILzJIJ6KE2WVDDy[YR2[3Srb36gZZN{[XluIFnDOVA:Oy5{zszN MmjNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEW3NVgoRjJ3M{C1O|E5RC:jPh?=
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RAW264.7 MXPGeY5kfGmxbjDhd5NigQ>? NF\1U3cyOCC3TR?= NYGw[4RrOC53IHjydy=> NULifXlkUW6qaXLpeIlwdiCxZjDNRXBMN06Ia3HwdIFDKGmwIFnDVkBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hVFCVLXnu[JVk\WRiSVy2JJBzd2S3Y4Tpc44h[XRiMUCgeW0heHKndILlZZRm\CCob4KgNE42KGi{czDmc4xtd3enZDDifUBNWFNiY3jhcIxmdmenIHHu[EBu\WG|dYLl[EBi\nSncjCyOEBpenNiYomgSWxKW0FicnXsZZRqfmVidH:gZ49vfHKxbB?= M1SxVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyN{iwNFg5Lz5|MEe4NFA5QDxxYU6=
BHK21 MmfiR5l1d3SxeHnjbZR6KGG|c3H5 M3rQblQ5KGi{cx?= MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBDUEt{MTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygR2M2OD12MD6xOO69VQ>? MoDIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzFyMEm5NFgoRjNzMEC5PVA5RC:jPh?=
SH-SY5Y MX7DfZRwfG:6aXPpeJkh[XO|YYm= M{K2TVczKGi{cx?= M3fUXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNJNVO\NWmgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD13Lkm0{txO NYXrRpczRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G0NFA4ODhpPkOxOFAxPzB6PD;hQi=>
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SH-SY5Y NIjSdZRHfW6ldHnvckBie3OjeR?= MU[xOUBucW6| Mn;jTY5pcWKrdHnvckBw\iCWcojSJIlvKGi3bXHuJHNJNVO\NWmgZ4VtdHNidYPpcochTFSQQjDhd{B{fWK|dILheIUheHKnaX7jeYJifGWmIH\vdkAyPSCvaX7zJIZwdGyxd3XkJIJ6KHO3YoP0doF1\SCjZHTpeIlwdiCjbnSgcYVie3W{ZXSg[o9zKDJyIH3pcpMh[nliRXzscYFvL3NibXX0bI9lNCCLQ{WwQVQ2Njh6zszN NFrQSWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUSwNFcxQCd-M{G0NFA4ODh:L3G+
Assay
Methods Test Index PMID
Western blot CDK2 / Cyclin E / Cyclin A ; Bax / Bcl-2 ; Survivin / p21 / p27 ; p-STAT3 / STAT3 / p-JAK2 / JAK2 / c-myc ; Hexokinase 1 / Hexokinase 2 ; p-AKT / AKT / p-S6 / S6 27634873 30906213
Growth inhibition assay Cell viability 25193861
In vivo Piperlongumine (50 mg/kg i.p.) causes in vivo growth inhibition of tumor cells without leading to major changes in the biochemical, hematological and histopathological parameters. [4]

Protocol (from reference)

Cell Research:

[3]

  • Cell lines: MCF-7 and 786-O cells
  • Concentrations: ~10 μM
  • Incubation Time: 48 hours
  • Method:

    MCF-7 and 786-O cells are incubated with various PL concentrations for 48h. Cell proliferation is analysed by CellTiter Blue assay. Effective doses (ED) are calculated using XLift, Microsoft Excel add-in.

Animal Research:

[4]

  • Animal Models: Mice transplanted with sarcoma 180 tumors
  • Dosages: ~50 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 317.34
Formula

C17H19NO5

CAS No. 20069-09-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=CC(=CC(=C1OC)OC)C=CC(=O)N2CCC=CC2=O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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