Piperlongumine

For research use only.

Catalog No.S7551 Synonyms: PPLGM, Piplartine

12 publications

Piperlongumine Chemical Structure

Molecular Weight(MW): 317.34

Piperlongumine, 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.

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Selleck's Piperlongumine has been cited by 12 publications

2 Customer Reviews

  • a. Cell growth of ARID1A-wildtype RMG1 cells transfected with ARID1A and non-target siRNA for 24 h and treated with piperlongumine for 72 h. b. Apoptosis of RMG1 cells after transfection and treatment as described in a as measured using annexin-V and PI staining. c. Cell growth of RMG1 cells transfected and treated with 5 μM of piperlongumine as described in a, but in the presence or absence of the antioxidant NAC. Cell growth was measured using the WST-1 assay and quantified relative to DMSO treated non-target control. *P < 0.05; **P < 0.01; ***P < 0.001.

    Oncotarget, 2016, 7(35):56933-56943. Piperlongumine purchased from Selleck.

    MPC cells were treated with the indicated concentrations of PL at 21% and 1% O2 for 24 hours. Total cell lysates were subjected to Western blot with antibodies against cleaved PARP, cleaved caspase 3, and caspase 3. β-tubulin was used as a loading control. A representative image (n=3) is shown.

    Oncotarget, 2016, 7(26):40531-40545. Piperlongumine purchased from Selleck.

Purity & Quality Control

Choose Selective ROS Inhibitors

Biological Activity

Description Piperlongumine, 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
MA9.3 cells NE\aOplEgXSxdH;4bYNqfHliYYPzZZk> NWHuXJBlPDhiaB?= MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNRVkvOyClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUKg{txO MoHqNlU1PjR6OEe=
mouse RAW264.7 cells M3r1[2Z2dmO2aX;uJIF{e2G7 M{W2U2FvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCOUGOtbY5lfWOnZDDOU{Bxem:mdXP0bY9vNCCLQ{WwQVMh|ryP M3POTFI2PDV|OEC5
PANC1 cells NH\pNWhEgXSxdH;4bYNqfHliYYPzZZk> M3r6flI1KGh? NWTyOG1uS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEGQQ{GgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEK0JIhzeyCkeTDNWHQhemWmdXP0bY9vKGG|c3H5MEBKSzVyPUOuNkDPxE1? MWSyOVMxPTdzOB?=
SK-MEL-2 cells NWjDflJyWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVLWXGpLPzJiaB?= NVn3bYFzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCHQ{WwQVQvOzlizszN M1:1OlI2QDJ4M{m4
HaCaT cells NYTiN3QxWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUK3NkBp NX\CWGV5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIZWNiXCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBGSzVyPUSuOFYh|ryP MlroNlU5OjZ|OUi=
ZR75-30 cells NYSyPFR4S3m2b4TvfIlkcXS7IHHzd4F6 NF7S[YU4OiCq MXnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDaVlc2NTNyIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OU45PiEQvF2= MXWyOFk{PzF6Nh?=
HCT116 cells M2rv[mN6fG:2b4jpZ4l1gSCjc4PhfS=> Mo\VO|IhcA>? NXr0XZlpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Pi5yNDFOwG0> MmDPNlQ6OzdzOE[=
A375 cells Mn7SVJJwdGmoZYLheIlwdiCjc4PhfS=> NGDDO4Q4OiCq M13o[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDFR|UxRTZwMUeg{txO NIHoZnYzPTh{NkO5PC=>
MDA-MB-231 cells NEe4OohEgXSxdH;4bYNqfHliYYPzZZk> MVW3NkBp MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:QC52NjFOwG0> MmLJNlQ6OzdzOE[=
A549 cells MnHDVJJwdGmoZYLheIlwdiCjc4PhfS=> M2m4T|czKGh? MnPsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFXDOVA:OTJwMjFOwG0> MWiyOVgzPjN7OB?=
HFF1 cells M1y3c3Bzd2yrZnXyZZRqd25iYYPzZZk> MWW3NkBp M{\sdGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgTGZHOSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBGSzVyPUGzMlEh|ryP MmP4NlU5OjZ|OUi=
MCF10A cells MofYVJJwdGmoZYLheIlwdiCjc4PhfS=> NVLO[lMxPzJiaB?= NYH3V4RDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2YyOEFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhTUN3ME2xPE4yKM7:TR?= NHribFgzPTh{NkO5PC=>
WI38 cells NGLFUIREgXSxdH;4bYNqfHliYYPzZZk> NFv5UpA4OiCq MYTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDXTVM5KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Mk[uO|gh|ryP NF\VdVYzPDl|N{G4Oi=>
MRC5 cells M3HadWN6fG:2b4jpZ4l1gSCjc4PhfS=> MnvVO|IhcA>? NEnrS4pEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOWkN3IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9N|UvODRizszN MmXYNlQ6OzdzOE[=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CDK2 / Cyclin E / Cyclin A ; 

PubMed: 27634873     


NCI-H929 cells were treated with 4 μM piperlongumine for 12, 24, or 48 h; cyclins and CDK2 levels were then measured

Bax / Bcl-2 ; 

PubMed: 27634873     


NCI-H929 cells were treated with 4 μM piperlongumine for 12 or 24 h and Bcl-2 and Bax levels were measured. Quantitative analysis was performed using Image J software, with normalization to GAPDH expression.

Survivin / p21 / p27 ; 

PubMed: 27634873     


NCI-H929 cells were treated with 4 μM piperlongumine for different amounts of time. Survivin, p21, and p27 levels were then measured.

p-STAT3 / STAT3 / p-JAK2 / JAK2 / c-myc ; 

PubMed: 27634873     


NCI-H929 cells were treated with 4 μM piperlongumine for different amounts of time, and STAT3, p-STAT3, p-JAK2, JAK2 and c-myc levels were then measured.

Hexokinase 1 / Hexokinase 2 ; 

PubMed: 30906213     


Piperlongumine regulates glycolysis in NSCLC cells. NSCLC cells, including H23 (A), HCC827 (B) and H1975 (C) were treated with different concentrations of piperlongumine for 24 h. Western blotting was performed to detect HK2 expression (left). The levels of glucose consumption (middle) and lactate production (right) were examined in these cells. Columns, mean of the number of colonies as determined from three independent experiments; bars, standard deviation; asterisk, significant (*p<0.05, **p<0.01, ***p<0.001) suppression of HK2 expression or glycolysis by piperlongumine compared with DMSO treated group. PL, Piperlongumine.

p-AKT / AKT / p-S6 / S6 ; 

PubMed: 30906213     


HCC827 (left), H1975 (middle) and H23 cells were treated with piperlongumine for 24 h, western blot was conducted to detect the target proteins as indicated.

27634873 30906213
Growth inhibition assay
Cell viability; 

PubMed: 25193861     


Piperlongumine induces death in HNC cells but not normal cells. Cytotoxicity was assessed by MTT assay 

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

Cell Research:

[3]

- Collapse
  • 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.


    (Only for Reference)
Animal Research:

[4]

- Collapse
  • Animal Models: Mice transplanted with sarcoma 180 tumors
  • Dosages: ~50 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 16 mg/mL warmed (50.41 mM)
Ethanol 6 mg/mL warmed (18.9 mM)
Water Insoluble
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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 317.34
Formula

C17H19NO5

CAS No. 20069-09-4
Storage powder
in solvent
Synonyms PPLGM, Piplartine
Smiles COC1=CC(=CC(=C1OC)OC)/C=C/C(=O)N2CCC=CC2=O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID