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別名: PPLGM, Piplartine 中文名稱:蓽茇酰胺
Piperlongumine (PPLGM, Piplartine),存在于胡椒科植物蓽茇中的一種天然生物堿,能夠增加reactive oxygen species (ROS)水平,并選擇性殺死癌細胞。它還是TrxR1的直接抑制劑,對胃癌具有抑制活性;一種新型的CRM1抑制劑;在人類乳腺癌細胞中可抑制PI3K/Akt/mTOR。
Piperlongumine Chemical Structure
CAS: 20069-09-4
相關(guān)產(chǎn)品 | MitoQ (Mitoquinone) mesylate H2DCFDA (DCFH-DA) Neohesperidin Carnosic acid Gallic acid (20R)Ginsenoside Rg3 Pyrogallol Idebenone Asiaticoside Sarsasapogenin Troxerutin | 點擊展開 |
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相關(guān)化合物庫 | 激酶抑制劑庫 FDA藥物庫 天然產(chǎn)物庫 已知活性藥物庫-I 高選擇性抑制劑庫 | 點擊展開 |
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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A549 | Function assay | 10 uM | 4 hrs | Reduction in total GSH level in human A549 cells at 10 uM after 4 hrs by luminescence assay | 25826398 |
A549 | Function assay | 10 uM | 4 hrs | Reduction in reduced GSH level in human A549 cells at 10 uM after 4 hrs by luminescence assay | 25826398 |
U937 | Apoptosis assay | 2 uM | 24 hrs | Induction of apoptosis in p53 null human U937 cells assessed as caspase 3 cleavage at 2 uM after 24 hrs in presence of SAHA by Western blot analysis | 27505848 |
U937 | Apoptosis assay | 2 uM | 24 hrs | Induction of apoptosis in p53 null human U937 cells assessed as PARP-1 cleavage at 2 uM after 24 hrs in presence of SAHA by Western blot analysis | 27505848 |
U937 | Cell death assay | 1 to 4 uM | 24 hrs | Induction of cell death in p53 null human U937 cells at 1 to 4 uM after 24 hrs by annexin V-FITC/PI staining based flow cytometry | 27505848 |
U937 | Cytotoxicity assay | 0.5 to 5 uM | 24 hrs | Cytotoxicity against p53 null human U937 cells assessed as decrease in cell viability at 0.5 to 5 uM after 24 hrs in presence of SAHA by MTT assay | 27505848 |
U937 | Function assay | 2 uM | 20 hrs | Induction of DNA damage in p53 null human U937 cells at 2 uM after 20 hrs in presence of SAHA by SYBR gold staining based alkaline comet assay | 27505848 |
MCF7 | Apoptosis assay | 10 uM | 48 hrs | Induction of apoptosis in human MCF7 cells assessed as downregulation of Bcl2 expression at 10 uM after 48 hrs by Western blot method | 27689728 |
MCF7 | Apoptosis assay | 10 uM | 72 hrs | Induction of apoptosis in human MCF7 cells assessed as downregulation of Mcl-1 expression at 10 uM after 72 hrs by Western blot method | 27689728 |
MCF7 | Function assay | 20 uM | 16 hrs | Disruption of microtubule network in human MCF7 cells at 20 uM after 16 hrs by immunofluorescence analysis | 27689728 |
MCF7 | Function assay | 10 uM | 16 hrs | Induction of microtubule depolymerization in human MCF7 cells at 10 uM after 16 hrs by immunofluorescence analysis | 27689728 |
MCF7 | Function assay | 1 to 20 uM | 48 hrs | Induction of reactive oxygen species generation in human MCF7 cells assessed as decrease in cell viability at 1 to 20 uM in presence of trolox after 48 hrs by alamarBlue assay | 27689728 |
MCF7 | Function assay | 5 to 20 uM | 4 hrs | Induction of tubulin depolymerization in human MCF7 cells at 5 to 20 uM after 4 hrs by Western blot method | 27689728 |
Jurkat | Function assay | 5 to 20 uM | 4 hrs | Induction of tubulin depolymerization in human Jurkat cells at 5 to 20 uM after 4 hrs by Western blot method | 27689728 |
HCT116 | Function assay | 10 uM | 1 hr | Induction of reactive oxygen species generation in human HCT116 cells at 10 uM after 1 hr by DCFH-DA dye-based fluorescence microscopic analysis | 28434764 |
HCT116 | Cell cycle assay | 1 to 5 uM | 24 hrs | Cell cycle arrest in human HCT116 cells assessed as accumulation at S phase 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method | 28434764 |
HCT116 | Cell cycle assay | 1 to 5 uM | 24 hrs | Cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method | 28434764 |
HCT116 | Cell cycle assay | 1 to 5 uM | 24 hrs | Cell cycle arrest in human HCT116 cells decrease in population at G0/G1 phase at 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method | 28434764 |
HCT116 | Antiproliferative assay | 10 uM | 72 hrs | Antiproliferative activity against human HCT116 cells at 10 uM after 72 hrs by MTT assay | 28686911 |
A549 | Antiproliferative assay | 10 uM | 72 hrs | Antiproliferative activity against human A549 cells at 10 uM after 72 hrs by MTT assay | 28686911 |
K562 | Antiproliferative assay | 10 uM | 72 hrs | Antiproliferative activity against human K562 cells at 10 uM after 72 hrs by MTT assay | 28686911 |
HCT116 | Antimigratory assay | 50 nM | 48 hrs | Antimigratory activity in human HCT116 cells assessed as inhibition of TGF-beta1-induced cell migration at 50 nM after 48 hrs by trans-well assay | 29424539 |
HCT116 | Function assay | 10 uM | 3 hrs | Induction of ROS accumulation in human HCT116 cells at 10 uM after 3 hrs by DCFH-DA staining-based fluorescence microscopic analysis | 29424539 |
HCT116 | Antiproliferative assay | 8 uM | 72 hrs | Antiproliferative activity against human HCT116 cells at 8 uM after 72 hrs by MTT assay | 29424539 |
HCT116 | Antiinvasive assay | 50 nM | 48 hrs | Antiinvasive activity in human HCT116 cells assessed as inhibition of TGF-beta1-induced cell invasion at 50 nM after 48 hrs by crystal violet staining-based assay | 29424539 |
HCT116 | Function assay | 50 nM | 1 hr | Inhibition of IL-1beta-mediated adhesion of human rhodamine 123-labeled HCT116 cells to HUVEC at 50 nM after 1 hr by fluoresence assay | 29424539 |
HCT116 | Function assay | 50 nM | 48 hrs | Inhibition of TGF-beta1-induced decrease in expression levels of E-cadherin protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 29424539 |
HCT116 | Function assay | 50 nM | 48 hrs | Inhibition of TGF-beta1-induced increase in expression levels of vimentin protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 29424539 |
HCT116 | Function assay | 50 nM | 48 hrs | Inhibition of TGF-beta1-induced increase in expression levels of MMP-9 protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 29424539 |
HCT116 | Function assay | 50 nM | 48 hrs | Inhibition of TGF-beta1-induced increase in expression levels of snail protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 29424539 |
HCT116 | Function assay | 50 nM | 48 hrs | Inhibition of TGF-beta1-induced increase in expression levels of twist protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 29424539 |
HCT116 | Function assay | 50 nM | 48 hrs | Inhibition of TGF-beta1-induced AKT phosphorylation in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 29424539 |
HCT116 | Function assay | 50 nM | 48 hrs | Inhibition of TGF-beta1-induced GSK-3beta phosphorylation in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 29424539 |
HCT116 | Function assay | 50 nM | 48 hrs | Inhibition of TGF-beta1-regulated decrease in cytoplasmic beta-catenin in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 29424539 |
HCT116 | Function assay | 50 nM | 48 hrs | Inhibition of TGF-beta1-regulated increase in nuclear beta-catenin in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 29424539 |
WI38 | Function assay | 5 uM | 24 hrs | Induction of OXR1 degradation in ionizing radiation induced human WI38 senescent cells at 5 uM after 24 hrs by Western blot analysis | 29925484 |
WI38 | Function assay | up to 64 uM | 1.5 hrs | Induction of ROS production in ionizing radiation induced human WI38 senescent cells up to 64 uM after 1.5 hrs by DHR123 dye based flow cytometry | 29925484 |
RAW264.7 | Function assay | 10 uM | 0.5 hrs | Inhibition of MAPK/NFkappaB in ICR mouse RAW264.7 cells assessed as reduction in LPS-induced TNFalpha production at 10 uM pretreated for 0.5 hrs followed by LPS challenge and measured after 24 hrs by ELISA relative to control | 30780088 |
RAW264.7 | Function assay | 10 uM | 0.5 hrs | Inhibition of MAPK/NFkappaB in ICR mouse RAW264.7 cells assessed as reduction in LPS-induced IL6 production at 10 uM pretreated for 0.5 hrs followed by LPS challenge and measured after 24 hrs by ELISA relative to control | 30780088 |
HaCaT | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HaCaT cells assessed as reduction in cell viability after 24 hrs by MTT reduction assay, IC50=16μM | 25305718 | |
PANC1 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human PANC1 cells assessed as reduction in cell viability after 24 hrs by MTT reduction assay, IC50=3.2μM | 25305718 | |
MRC5 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, IC50=35.04μM | 24937186 | |
WI38 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human WI38 cells after 72 hrs by MTT assay, IC50=26.78μM | 24937186 | |
A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=22.85μM | 24937186 | |
MDA-MB-231 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=8.46μM | 24937186 | |
HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=6.04μM | 24937186 | |
ZR75-30 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human ZR75-30 cells after 72 hrs by MTT assay, IC50=5.86μM | 24937186 | |
MA9.3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MA9.3 cells after 48 hrs by MTT assay, IC50=2μM | 25464887 | |
SK-MEL-2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by MTT assay, EC50=4.39μM | 25826398 | |
HaCaT | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HaCaT cells after 72 hrs by MTT assay, EC50=4.46μM | 25826398 | |
A375 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A375 cells after 72 hrs by MTT assay, EC50=6.17μM | 25826398 | |
HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, EC50=11.5μM | 25826398 | |
A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, EC50=12.2μM | 25826398 | |
HFF1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against HFF1 cells after 72 hrs by MTT assay, EC50=13.1μM | 25826398 | |
MCF10A | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay, EC50=18.1μM | 25826398 | |
A549 | Function assay | 3 hrs | Induction of ROS production in human A549 cells after 3 hrs by DHE staining-based fluorescence assay | 25826398 | |
A549 | Function assay | 3 hrs | Induction of ROS production in human A549 cells after 3 hrs by APF staining-based fluorescence assay | 25826398 | |
HT1080 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HT1080 cells assessed as cell viability after 72 hrs by resazurin reduction assay, IC50=3.43μM | 26599530 | |
GBM10 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human GBM10 cells assessed as cell viability after 72 hrs by resazurin reduction assay, IC50=3.81μM | 26599530 | |
SF188 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SF188 cells assessed as cell viability after 72 hrs by resazurin reduction assay, IC50=3.9μM | 26599530 | |
SKBR3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SKBR3 cells assessed as cell viability after 72 hrs by resazurin reduction assay, IC50=4.04μM | 26599530 | |
T98G | Cytotoxicity assay | 72 hrs | Cytotoxicity against human T98G cells assessed as cell viability after 72 hrs by resazurin reduction assay, IC50=4.92μM | 26599530 | |
HT-29 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HT-29 cells assessed as cell viability after 72 hrs by resazurin reduction assay, IC50=5.49μM | 26599530 | |
MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells assessed as cell viability after 72 hrs by resazurin reduction assay, IC50=6.14μM | 26599530 | |
A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by resazurin reduction assay, IC50=6.54μM | 26599530 | |
MV4-11 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MV4-11 cells after 72 hrs in presence of SAHA by MTT assay, IC50=0.2891μM | 27505848 | |
CMK | Antiproliferative assay | 72 hrs | Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs in presence of SAHA by MTT assay, IC50=0.4218μM | 27505848 | |
CMY | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CMY cells after 72 hrs in presence of SAHA by MTT assay, IC50=0.4424μM | 27505848 | |
HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells after 72 hrs in presence of SAHA by MTT assay, IC50=0.5292μM | 27505848 | |
CMK | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CMK cells after 72 hrs in presence of SAHA by MTT assay, IC50=0.6127μM | 27505848 | |
U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against p53 null human U937 cells after 72 hrs in presence of SAHA by MTT assay, IC50=0.767μM | 27505848 | |
MOLM13 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs in presence of SAHA by MTT assay, IC50=0.9345μM | 27505848 | |
CMS | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CMS cells after 72 hrs in presence of SAHA by MTT assay, IC50=1.037μM | 27505848 | |
OCI-AML3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human OCI-AML3 cells after 72 hrs in presence of SAHA by MTT assay, IC50=1.109μM | 27505848 | |
HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs in presence of SAHA by MTT assay, IC50=1.128μM | 27505848 | |
MV4-11 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay, IC50=1.439μM | 27505848 | |
CMY | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CMY cells after 72 hrs by MTT assay, IC50=1.62μM | 27505848 | |
HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=1.778μM | 27505848 | |
MOLM13 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs by MTT assay, IC50=1.838μM | 27505848 | |
OCI-AML3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay, IC50=1.868μM | 27505848 | |
CMK | Antiproliferative assay | 72 hrs | Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs by MTT assay, IC50=1.911μM | 27505848 | |
U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against p53 null human U937 cells after 72 hrs by MTT assay, IC50=2.174μM | 27505848 | |
HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs by MTT assay, IC50=2.25μM | 27505848 | |
CMK | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CMK cells after 72 hrs by MTT assay, IC50=2.815μM | 27505848 | |
CMS | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CMS cells after 72 hrs by MTT assay, IC50=3.097μM | 27505848 | |
MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity in human MCF7 cells assessed as cell viability after 48 hrs by alamarBlue assay, IC50=1.2μM | 27689728 | |
Jurkat | Antiproliferative assay | 48 hrs | Antiproliferative activity in human Jurkat cells assessed as cell viability after 48 hrs by alamarBlue assay, IC50=1.4μM | 27689728 | |
Jurkat | Cytotoxicity assay | 24 hrs | Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay, IC50=5μM | 27689728 | |
MCF7 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay, IC50=8μM | 27689728 | |
A549 | Function assay | 24 hrs | Inhibition of NF-kappaB in human A549 cells after 24 hrs by luciferase reporter gene assay, IC50=1.76μM | 27810594 | |
HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=8.9μM | 28159415 | |
HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=9.2μM | 28159415 | |
A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=10μM | 28159415 | |
MRC5 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, IC50=37μM | 28159415 | |
A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=6.84μM | 28434764 | |
Saos2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Saos2 cells after 72 hrs by MTT assay, IC50=7.31μM | 28434764 | |
HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=7.34μM | 28434764 | |
U2OS | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U2OS cells after 72 hrs by MTT assay, IC50=9.49μM | 28434764 | |
MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=10.6μM | 28434764 | |
SKHEP1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SKHEP1 cells after 72 hrs by MTT assay, IC50=13.3μM | 28434764 | |
HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50=2.65μM | 28686911 | |
HCT8 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay, IC50=4.1μM | 28686911 | |
HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=8.13μM | 28686911 | |
CCD-841 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human CCD-841 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=44.32μM | 28686911 | |
HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50=2.65μM | 29424539 | |
HCT8 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay, IC50=4.1μM | 29424539 | |
SW620 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay, IC50=4.62μM | 29424539 | |
K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50=5.05μM | 29424539 | |
K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells after 72 hrs in presence of ligustrazine by MTT assay, IC50=5.09μM | 29424539 | |
HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=8.13μM | 29424539 | |
HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs in presence of ligustrazine by MTT assay, IC50=8.17μM | 29424539 | |
A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs in presence of ligustrazine by MTT assay, IC50=15.22μM | 29424539 | |
A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=15.28μM | 29424539 | |
U87MG | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U87MG cells after 72 hrs in presence of ligustrazine by MTT assay, IC50=16.15μM | 29424539 | |
U87MG | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay, IC50=17.34μM | 29424539 | |
CCD-841 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CCD-841 cells after 72 hrs by MTT assay, IC50=44.32μM | 29424539 | |
DU145 | Function assay | 24 hrs | Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells after 24 hrs by Western blot analysis, IC50=7μM | 29807795 | |
DU145 | Growth inhibition assay | 48 hrs | Growth inhibition of human DU145 cells after 48 hrs by WST-1 assay, GI50=7.1μM | 29807795 | |
LNCAP | Growth inhibition assay | 48 hrs | Growth inhibition of human LNCAP cells after 48 hrs by WST-1 assay, GI50=9.2μM | 29807795 | |
BHK21 | Cytotoxicity assay | 48 hrs | Cytotoxicity against BHK21 cells assessed as reduction in cell viability after 48 hrs by MTT assay, CC50=40.14μM | 31009908 | |
SH-SY5Y | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=5.94μM | 31400708 | |
U87 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=7.18μM | 31400708 | |
SH-SY5Y | Function assay | 15 mins | Inhibition of TrxR in human SH-SY5Y cells using DTNB as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by Ellman's method, IC50=45.88μM | 31400708 | |
RAW264.7 | Antiinflammatory assay | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production, IC50=3μM | 25453809 | ||
WI38 | Function assay | Senolytic activity against ionizing radiation induced human WI38 senescent cells assessed as reduction in cell viability by propidium iodide staining based flow cytometry, EC50=8μM | 29925484 | ||
WI38 | Function assay | Senolytic activity against non-senescent human WI38 cells assessed as reduction in cell viability by propidium iodide staining based flow cytometry, EC50=20.3μM | 29925484 | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | Piperlongumine (PPLGM, Piplartine),存在于胡椒科植物蓽茇中的一種天然生物堿,能夠增加reactive oxygen species (ROS)水平,并選擇性殺死癌細胞。它還是TrxR1的直接抑制劑,對胃癌具有抑制活性;一種新型的CRM1抑制劑;在人類乳腺癌細胞中可抑制PI3K/Akt/mTOR。 | ||||
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | Piperlongumine是一種已知的ROS誘導(dǎo)劑,可誘導(dǎo)胰腺癌細胞的細胞死亡[2]。作為一種血栓素A(2)受體拮抗劑,Piperlongumine抑制血小板聚集。[2] Piperlongumine也能夠通過抑制Akt/mTOR信號通路促進細胞自噬,并介導(dǎo)腫瘤細胞死亡。[3] | |||
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細胞實驗 | 細胞系 | MCF-7 和 786-O 細胞 | ||
濃度 | ~10?μM | |||
孵育時間 | 48小時 | |||
方法 | MCF-7和786-O細胞與不同濃度的PL培養(yǎng)48小時。細胞增殖通過CellTiter Blue測試分析。有效劑量(ED)使用XLift,Microsoft Excel加載項計算。 |
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實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
Western blot | CDK2 / Cyclin E / Cyclin A Bax / Bcl-2 Survivin / p21 / p27 p-STAT3 / STAT3 / p-JAK2 / JAK2 / c-myc Hexokinase 1 / Hexokinase 2 p-AKT / AKT / p-S6 / S6 |
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27634873 | |
Growth inhibition assay | Cell viability |
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25193861 |
體內(nèi)研究(In Vivo) | ||
體內(nèi)研究活性 | Piperlongumine (50 mg/kg i.p.)引起體內(nèi)腫瘤細胞的生長抑制,而不改變生物化學(xué),血液學(xué)和組織病理學(xué)參數(shù)。[4] | |
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動物實驗 | Animal Models | 移植肉瘤 180 腫瘤的小鼠 |
Dosages | ~50 mg/kg | |
Administration | i.p. |
分子量 | 317.34 | 分子式 | C17H19NO5 |
CAS號 | 20069-09-4 | SDF | Download Piperlongumine SDF |
Smiles | COC1=CC(=CC(=C1OC)OC)C=CC(=O)N2CCC=CC2=O | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 63 mg/mL ( (198.52 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Ethanol : 63 mg/mL (198.52 mM) Water : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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