Piperlongumine

For research use only. Not for use in humans.

目录号:S7551 别名: PPLGM, Piplartine

Piperlongumine Chemical Structure

CAS No. 20069-09-4

Piperlongumine (PPLGM, Piplartine),存在于胡椒科植物荜茇中的一种天然生物碱,能够增加reactive oxygen species (ROS)水平,并选择性杀死癌细胞。它还是TrxR1的直接抑制剂,对胃癌具有抑制活性;一种新型的CRM1抑制剂;在人类乳腺癌细胞中可抑制PI3K/Akt/mTOR

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客户使用Selleck生产的Piperlongumine发表文献14篇:

客户使用该产品的2个实验数据:

  • 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.

产品安全说明书

ROS抑制剂选择性比较

生物活性

产品描述 Piperlongumine (PPLGM, Piplartine),存在于胡椒科植物荜茇中的一种天然生物碱,能够增加reactive oxygen species (ROS)水平,并选择性杀死癌细胞。它还是TrxR1的直接抑制剂,对胃癌具有抑制活性;一种新型的CRM1抑制剂;在人类乳腺癌细胞中可抑制PI3K/Akt/mTOR
靶点
reactive oxygen species (ROS) [1] TrxR1 [5] CRM1 [6] PI3K/Akt/mTOR [7]
体外研究

Piperlongumine是一种已知的ROS诱导剂,可诱导胰腺癌细胞的细胞死亡[2]。作为一种血栓素A(2)受体拮抗剂,Piperlongumine抑制血小板聚集。[2] Piperlongumine也能够通过抑制Akt/mTOR信号通路促进细胞自噬,并介导肿瘤细胞死亡。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MA9.3 cells MULDfZRwfG:6aXPpeJkh[XO|YYm= M4iwTlQ5KGh? MnruR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWE6NjNiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2yJO69VQ>? M2mwcVI2PDZ2OEi3
mouse RAW264.7 cells M1vQ[mZ2dmO2aX;uJIF{e2G7 Mk\vRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDpckBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEySUz3pcoR2[2WmIF7PJJBzd2S3Y4Tpc44tKEmFNUC9N{DPxE1? NEWzUZAzPTR3M{iwPS=>
PANC1 cells M3;LfGN6fG:2b4jpZ4l1gSCjc4PhfS=> NGLk[3QzPCCq M{HCR2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBCVkNzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB{NDDodpMh[nliTWTUJJJm\HWldHnvckBie3OjeTygTWM2OD1|LkKg{txO NILPOmszPTNyNUexPC=>
SK-MEL-2 cells MX3Qdo9tcW[ncnH0bY9vKGG|c3H5 M4DTWlczKGh? NETzc3VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC1{IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEWFNUC9OE4{QSEQvF2= MnLQNlU5OjZ|OUi=
HaCaT cells NVTjc|hMWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUS3NkBp MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEijQ3HUJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFXDOVA:PC52NjFOwG0> NXfQbm9QOjV6Mk[zPVg>
ZR75-30 cells MkfOR5l1d3SxeHnjbZR6KGG|c3H5 MX23NkBp MULDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDaVlc2NTNyIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OU45PiEQvF2= M{PwN|I1QTN5MUi2
HCT116 cells NWTRPIxPS3m2b4TvfIlkcXS7IHHzd4F6 NY\oN2pTPzJiaB?= MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME22MlA1KM7:TR?= M2XFNVI1QTN5MUi2
A375 cells MYTQdo9tcW[ncnH0bY9vKGG|c3H5 NWnnZ49tPzJiaB?= NUG2T5Z6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGVEPTB;Nj6xO{DPxE1? MmrJNlU5OjZ|OUi=
MDA-MB-231 cells NGDiXFNEgXSxdH;4bYNqfHliYYPzZZk> NEfyXWE4OiCq MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:QC52NjFOwG0> MXOyOFk{PzF6Nh?=
A549 cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 M4fZTFczKGh? MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiRVO1NF0yOi5{IN88US=> NVq5[HhXOjV6Mk[zPVg>
HFF1 cells NHK3boZRem:uaX\ldoF1cW:wIHHzd4F6 M4rUdlczKGh? Mkf2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDISmYyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGVEPTB;MUOuNUDPxE1? M{LnUFI2QDJ4M{m4
MCF10A cells MVzQdo9tcW[ncnH0bY9vKGG|c3H5 NFe1UGo4OiCq MnT6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[xNGEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygSWM2OD1zOD6xJO69VQ>? NV3EXY9tOjV6Mk[zPVg>
WI38 cells Mn;JR5l1d3SxeHnjbZR6KGG|c3H5 NYDiOGZnPzJiaB?= M4fSfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHdKOzhiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2yOk44QCEQvF2= NIjW[4ozPDl|N{G4Oi=>
MRC5 cells MlnwR5l1d3SxeHnjbZR6KGG|c3H5 NVLxVVEyPzJiaB?= MljlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUO1MlA1KM7:TR?= NUH2VZlzOjR7M{exPFY>

... 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
体内研究 Piperlongumine (50 mg/kg i.p.)引起体内肿瘤细胞的生长抑制,而不改变生物化学,血液学和组织病理学参数。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[3]

- 合并
  • Cell lines: MCF-7 和 786-O 细胞
  • Concentrations: ~10 μM
  • Incubation Time: 48小时
  • Method:

    MCF-7和786-O细胞与不同浓度的PL培养48小时。细胞增殖通过CellTiter Blue测试分析。有效剂量(ED)使用XLift,Microsoft Excel加载项计算。


    (Only for Reference)
动物实验:

[4]

- 合并
  • Animal Models: 移植肉瘤 180 肿瘤的小鼠
  • Dosages: ~50 mg/kg
  • Administration: i.p.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 16 mg/mL warmed (50.41 mM)
Water Insoluble
Ethanol '6 mg/mL warmed
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 317.34
化学式

C17H19NO5

CAS号 20069-09-4
储存条件 粉状
溶于溶剂
别名 PPLGM, Piplartine

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID