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 MYrDfZRwfG:6aXPpeJkh[XO|YYm= MlHoOFghcA>? NGfYR5NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOSTlwMzDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVIh|ryP NF\iVYkzPTR4NEi4Oy=>
mouse RAW264.7 cells M4TWfWZ2dmO2aX;uJIF{e2G7 NIjXSVBCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKG2xdYPlJHJCXzJ4ND63JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdixiSVO1NF0{KM7:TR?= M1PmdFI2PDV|OEC5
PANC1 cells NXXzeXlqS3m2b4TvfIlkcXS7IHHzd4F6 NX3rXGM4OjRiaB?= MkjJR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGFPSzFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDJ2IHjyd{BjgSCPVGSgdoVlfWO2aX;uJIF{e2G7LDDJR|UxRTNwMjFOwG0> M3i3ZlI2OzB3N{G4
SK-MEL-2 cells NFT2VnlRem:uaX\ldoF1cW:wIHHzd4F6 NFrmbnQ4OiCq Ml7GRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuOiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBGSzVyPUSuN|kh|ryP NGLLVpQzPTh{NkO5PC=>
HaCaT cells MlrHVJJwdGmoZYLheIlwdiCjc4PhfS=> MYe3NkBp NHrq[2pCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjhR4FVKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGVEPTB;ND60OkDPxE1? MoTBNlU5OjZ|OUi=
ZR75-30 cells NGXYVJBEgXSxdH;4bYNqfHliYYPzZZk> Mm\nO|IhcA>? NIH6emFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBbWjd3LUOwJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PS56NjFOwG0> NXizbWJFOjR7M{exPFY>
HCT116 cells M2fCRmN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml;GO|IhcA>? NGXjdWZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF03NjB2IN88US=> NIH1bmgzPDl|N{G4Oi=>
A375 cells M2LSNXBzd2yrZnXyZZRqd25iYYPzZZk> NYCxUm5VPzJiaB?= MlHhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFXDOVA:Pi5zNzFOwG0> NVn1SZB1OjV6Mk[zPVg>
MDA-MB-231 cells M2XNTGN6fG:2b4jpZ4l1gSCjc4PhfS=> MnzjO|IhcA>? Mlr4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRThwNE[g{txO M{K1fFI1QTN5MUi2
A549 cells MYfQdo9tcW[ncnH0bY9vKGG|c3H5 MYG3NkBp M1XvcGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDFR|UxRTF{LkKg{txO M33DZVI2QDJ4M{m4
HFF1 cells NWP4Z2lDWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXHMeYRVPzJiaB?= MUjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFjGSlEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygSWM2OD1zMz6xJO69VQ>? MoLCNlU5OjZ|OUi=
MCF10A cells NHnnNYVRem:uaX\ldoF1cW:wIHHzd4F6 M4\CfVczKGh? MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkGwRUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDFR|UxRTF6LkGg{txO MYSyOVgzPjN7OB?=
WI38 cells MnHHR5l1d3SxeHnjbZR6KGG|c3H5 Mke1O|IhcA>? NYm2eJJqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hX0l|ODDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVI3Njd6IN88US=> NIfEfGgzPDl|N{G4Oi=>
MRC5 cells MlnZR5l1d3SxeHnjbZR6KGG|c3H5 MUS3NkBp M2r5PWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1TSzViY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2zOU4xPCEQvF2= MkHaNlQ6OzdzOE[=

... 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
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

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID