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Piperlongumine ROS chemisch

Name: Piperlongumine
Brand: Selleck Chemicals
SKU: S7551
Rating: 5 (30 reviews)

Cat.Nr.S7551

Piperlongumine (PPLGM, Piplartine), een natuurlijke alkaloïde uit Piper longum L., verhoogt het niveau van reactieve zuurstofsoorten (ROS) en doodt selectief kankercellen. Het is een directe TrxR1-remmer met onderdrukkende activiteit tegen maagkanker en een nieuwe remmer van CRM1; ook een remmer van PI3K/Akt/mTOR in menselijke borstkankercellen.

Piperlongumine ROS chemisch Chemical Structure

Chemische structuur

Moleculair gewicht: 317.34

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Kwaliteitscontrole

Batch: Zuiverheid: 99.33%

99.33

Gerelateerde doelwitten	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Overige ROS Inhibitoren	MitoQ (Mitoquinone) Mesylate H2DCFDA (DCFH-DA) Neohesperidin Gallic acid Idebenone Carnosic acid Pyrogallol (20R)Ginsenoside Rg3 Troxerutin Sarsasapogenin

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
ZR75-30	Cytotoxicity assay		72 hrs	Cytotoxicity against human ZR75-30 cells after 72 hrs by MTT assay, IC50=5.86μM	24937186
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=6.04μM	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
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=22.85μM	24937186
WI38	Cytotoxicity assay		72 hrs	Cytotoxicity against human WI38 cells after 72 hrs by MTT assay, IC50=26.78μM	24937186
MRC5	Cytotoxicity assay		72 hrs	Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, IC50=35.04μM	24937186
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
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
RAW264.7	Antiinflammatory assay			Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production, IC50=3μM	25453809
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
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
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
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	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
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
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
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
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
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
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
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
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
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
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
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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	317.34	Formule	C₁₇H₁₉NO₅	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	20069-09-4	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	PPLGM, Piplartine			Smiles	COC1=CC(=CC(=C1OC)OC)C=CC(=O)N2CCC=CC2=O

Oplosbaarheid

In vitro
Batch:

DMSO : 63 mg/mL (198.52 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 63 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	reactive oxygen species (ROS) TrxR1 CRM1 PI3K/Akt/mTOR
In vitro	Piperlongumine is een bekende ROS-inductor die de dood van alvleesklierkankercellen in celcultuur kan induceren Als een tromboxaan A(2)-receptorantagonist remt deze verbinding de plaatjesaggregatie. Het bevordert ook autofagie via remming van Akt/mTOR-signalering en medieert de dood van kankercellen.
In vivo	Piperlongumine (50 mg/kg i.p.) veroorzaakt in vivo groeiremming van tumorcellen zonder te leiden tot grote veranderingen in de biochemische, hematologische en histopathologische parameters.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/25530945/ [2] https://pubmed.ncbi.nlm.nih.gov/17618620/ [3] https://pubmed.ncbi.nlm.nih.gov/24853732/ [4] https://pubmed.ncbi.nlm.nih.gov/17975786/ [5] https://pubmed.ncbi.nlm.nih.gov/26963494/ [6] https://pubmed.ncbi.nlm.nih.gov/26026911/ [7] https://pubmed.ncbi.nlm.nih.gov/24729100/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	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

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