Piperlongumine

Catalog No.S7551 Synonyms: PPLGM, Piplartine

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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  • 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 Ml;iR5l1d3SxeHnjbZR6KGG|c3H5 NEjYcWQ1QCCq M2Hve2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1CQS5|IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NkDPxE1? NGW4[|AzPTR4NEi4Oy=>
mouse RAW264.7 cells MVfGeY5kfGmxbjDhd5NigQ>? MnTiRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDpckBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEySUz3pcoR2[2WmIF7PJJBzd2S3Y4Tpc44tKEmFNUC9N{DPxE1? NX\3WJgxOjV2NUO4NFk>
PANC1 cells M{\zPWN6fG:2b4jpZ4l1gSCjc4PhfS=> NFvG[ZUzPCCq M3vK[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBCVkNzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB{NDDodpMh[nliTWTUJJJm\HWldHnvckBie3OjeTygTWM2OD1|LkKg{txO NF\ScGEzPTNyNUexPC=>
SK-MEL-2 cells M{m3[XBzd2yrZnXyZZRqd25iYYPzZZk> NIXIdIk4OiCq NGPUPHlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC1{IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEWFNUC9OE4{QSEQvF2= NE\jOHAzPTh{NkO5PC=>
HaCaT cells MnnYVJJwdGmoZYLheIlwdiCjc4PhfS=> MkXHO|IhcA>? MoDuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKYVPhWEBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDFR|UxRTRwNE[g{txO MnvlNlU5OjZ|OUi=
ZR75-30 cells Mm\4R5l1d3SxeHnjbZR6KGG|c3H5 MYK3NkBp M2K3eGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHpTPzVvM{CgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF02Njh4IN88US=> MnnFNlQ6OzdzOE[=
HCT116 cells M3H0SWN6fG:2b4jpZ4l1gSCjc4PhfS=> Mor2O|IhcA>? MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME22MlA1KM7:TR?= MYSyOFk{PzF6Nh?=
A375 cells MkK0VJJwdGmoZYLheIlwdiCjc4PhfS=> M3LHbFczKGh? Mn24RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFXDOVA:Pi5zNzFOwG0> M1L6V|I2QDJ4M{m4
MDA-MB-231 cells MkDJR5l1d3SxeHnjbZR6KGG|c3H5 NH61dWQ4OiCq MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:QC52NjFOwG0> M1;me|I1QTN5MUi2
A549 cells M1;R[nBzd2yrZnXyZZRqd25iYYPzZZk> NFXDOos4OiCq NEXxRWFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygSWM2OD1zMj6yJO69VQ>? M1LldlI2QDJ4M{m4
HFF1 cells NWfrS2ZQWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVyzO4J4PzJiaB?= MnLTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDISmYyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGVEPTB;MUOuNUDPxE1? Mnf2NlU5OjZ|OUi=
MCF10A cells NGLxepJRem:uaX\ldoF1cW:wIHHzd4F6 NELyWZk4OiCq M1HkdGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGNVBCKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGVEPTB;MUiuNUDPxE1? M3r5W|I2QDJ4M{m4
WI38 cells MXzDfZRwfG:6aXPpeJkh[XO|YYm= MkDRO|IhcA>? NEjFOmNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBYUTN6IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NlYvPzhizszN M2OxS|I1QTN5MUi2
MRC5 cells NVyxflVpS3m2b4TvfIlkcXS7IHHzd4F6 NVvZR45yPzJiaB?= MnzzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUO1MlA1KM7:TR?= NYXqXmtxOjR7M{exPFY>

... Click to View More Cell Line Experimental Data

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]

+ Expand
  • 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]

+ Expand
  • Animal Models: Mice transplanted with sarcoma 180 tumors
  • Formulation: 4% DMSO
  • 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

* 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
Synonyms PPLGM, Piplartine

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID