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 MlLkR5l1d3SxeHnjbZR6KGG|c3H5 NF30bno1QCCq MmP6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWE6NjNiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2yJO69VQ>? NWXpOpdNOjV2NkS4PFc>
mouse RAW264.7 cells Ml;jSpVv[3Srb36gZZN{[Xl? NIGwSI9CdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKG2xdYPlJHJCXzJ4ND63JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdixiSVO1NF0{KM7:TR?= MnLuNlU1PTN6MEm=
PANC1 cells MnLPR5l1d3SxeHnjbZR6KGG|c3H5 M1PTN|I1KGh? NFzwbYxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSU6FMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiMkSgbJJ{KGK7IF3UWEBz\WS3Y4Tpc44h[XO|YYmsJGlEPTB;Mz6yJO69VQ>? MX6yOVMxPTdzOB?=
SK-MEL-2 cells NIjFOXFRem:uaX\ldoF1cW:wIHHzd4F6 NI\qe5o4OiCq NXrVXY85SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCHQ{WwQVQvOzlizszN M1u5cFI2QDJ4M{m4
HaCaT cells M4Cw[HBzd2yrZnXyZZRqd25iYYPzZZk> Mm\mO|IhcA>? NHnmcVFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjhR4FVKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGVEPTB;ND60OkDPxE1? MnW2NlU5OjZ|OUi=
ZR75-30 cells MkDJR5l1d3SxeHnjbZR6KGG|c3H5 M1LNPFczKGh? MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDaVlc2NTNyIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OU45PiEQvF2= M3\z[|I1QTN5MUi2
HCT116 cells NVjJc5pZS3m2b4TvfIlkcXS7IHHzd4F6 M2DsXFczKGh? Ml3xR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9Ok4xPCEQvF2= NIPLR5IzPDl|N{G4Oi=>
A375 cells NIXlS2ZRem:uaX\ldoF1cW:wIHHzd4F6 MlT1O|IhcA>? NWLVSHhZSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGVEPTB;Nj6xO{DPxE1? MmrrNlU5OjZ|OUi=
MDA-MB-231 cells M2nST2N6fG:2b4jpZ4l1gSCjc4PhfS=> NUL2OZppPzJiaB?= MoXqR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRThwNE[g{txO MmrPNlQ6OzdzOE[=
A549 cells NVT3cHpbWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWKxbXM3PzJiaB?= NWW0dpQySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGVEPTB;MUKuNkDPxE1? NETlfmgzPTh{NkO5PC=>
HFF1 cells NWfTcpFPWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUPs[45sPzJiaB?= NFnoXmxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGhHTjFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhTUN3ME2xN{4yKM7:TR?= M{HvUVI2QDJ4M{m4
MCF10A cells NVvKPHVRWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXLYUHR3PzJiaB?= MnjERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[xNGEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygSWM2OD1zOD6xJO69VQ>? MoL1NlU5OjZ|OUi=
WI38 cells NIHlfVFEgXSxdH;4bYNqfHliYYPzZZk> NYr5d4ozPzJiaB?= MoOxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gW2k{QCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUK2Mlc5KM7:TR?= NHf3R4EzPDl|N{G4Oi=>
MRC5 cells M{PWSGN6fG:2b4jpZ4l1gSCjc4PhfS=> NIPa[|A4OiCq M3jBSmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1TSzViY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2zOU4xPCEQvF2= MX2yOFk{PzF6Nh?=

... 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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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID