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Piperlongumine

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

Piperlongumine Chemical Structure

CAS: 20069-09-4

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 958.23 現(xiàn)貨
10mg 790.72 現(xiàn)貨
50mg 2911.49 現(xiàn)貨
200mg 7749.45 現(xiàn)貨
1g 16134.3 現(xiàn)貨
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Piperlongumine相關(guān)產(chǎn)品

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

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。
靶點
reactive oxygen species (ROS) [1] TrxR1 [5] CRM1 [6] PI3K/Akt/mTOR [7]
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]
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。

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 27634873
Growth inhibition assay Cell viability 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]
動物實驗 Animal Models 移植肉瘤 180 腫瘤的小鼠
Dosages ~50 mg/kg
Administration i.p.

化學(xué)信息&溶解度

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
批次:

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
批次:

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

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

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)

mg/kg g μL

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)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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,: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: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: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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