Piperlongumine (Synonyms: Piplartine)

Name: Piperlongumine
Brand: MedChemExpress
SKU: HY-N2329
Rating: 5.0 (8 reviews)

Cat. No.: HY-N2329 Purity: 99.87%: FAQs
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Piperlongumine is a alkaloid, possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway. Piperlongumin could be used in the study of migrasome.

For research use only. We do not sell to patients.

Piperlongumine Chemical Structure

CAS No. : 20069-09-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

7 Publications Citing Use of MCE Piperlongumine

•Original Article. 2022.

: Piperlongumine purchased from MedChemExpress. Usage Cited in: Original Article. 2022.; Piperlongumine (PL) affectes the expression of ferroptosis related proteins in OSCC cells. PL (6, 12, 24 h) increases the expression of DMT1 in OSCC cells, and decreases the expression of FTH1, SLC7A11 and GPX4.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Piperlongumine is a alkaloid^[1], possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities^[2]. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines^[1]. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway. Piperlongumin could be used in the study of migrasome^[2]^[3].

IC₅₀ & Target^[2]

ERK1

ERK2

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	EC₅₀	6.17 μM Compound: piperlongumine	Antiproliferative activity against human A375 cells after 72 hrs by MTT assay Antiproliferative activity against human A375 cells after 72 hrs by MTT assay	[PMID: 25826398]
A549	ED₅₀	0.6 μg/mL Compound: 3	Cytotoxicity against human A549 cells after 6 days by MTT assay Cytotoxicity against human A549 cells after 6 days by MTT assay	[PMID: 2089124]
A549	IC₅₀	1.76 μM Compound: Piperlongumine	Inhibition of NF-kappaB in human A549 cells after 24 hrs by luciferase reporter gene assay Inhibition of NF-kappaB in human A549 cells after 24 hrs by luciferase reporter gene assay	[PMID: 27810594]
A549	IC₅₀	10 μM Compound: 1; PL	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 28159415]
A549	EC₅₀	12.2 μM Compound: piperlongumine	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 25826398]
A549	IC₅₀	15.22 μM Compound: 1	Antiproliferative activity against human A549 cells after 72 hrs in presence of ligustrazine by MTT assay Antiproliferative activity against human A549 cells after 72 hrs in presence of ligustrazine by MTT assay	[PMID: 29424539]
A549	IC₅₀	15.28 μM Compound: 1	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 29424539]
A549	IC₅₀	22.85 μM Compound: PL	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 24937186]
A549	IC₅₀	3.2 μM Compound: 1; PL	Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay	[PMID: 32736231]
A549	IC₅₀	6.54 μM Compound: PL	Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by resazurin reduction assay Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by resazurin reduction assay	[PMID: 26599530]
A549	IC₅₀	6.84 μM Compound: PL	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 28434764]
Bel-7402	IC₅₀	5.6 μM Compound: 1	Antiproliferative activity against human Bel-7402 cells incubated for 24 hrs by MTT assay Antiproliferative activity against human Bel-7402 cells incubated for 24 hrs by MTT assay	[PMID: 34806369]
Bel-7402	IC₅₀	5.6 μM Compound: PL	Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33026807]
Bel7402/5-FU	IC₅₀	8.4 μM Compound: 1	Antiproliferative activity against human BEL-7402/5-FU cells incubated for 24 hrs by MTT assay Antiproliferative activity against human BEL-7402/5-FU cells incubated for 24 hrs by MTT assay	[PMID: 34806369]
Bel7402/5-FU	IC₅₀	8.4 μM Compound: PL	Cytotoxicity against human BEL-7402/5-FU cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human BEL-7402/5-FU cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33026807]
BHK-21	CC₅₀	40.14 μM Compound: Piplartine	Cytotoxicity against BHK21 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against BHK21 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31009908]
CMK	IC₅₀	1911 nM Compound: PL	Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs by MTT assay Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs by MTT assay	[PMID: 27505848]
CMK	IC₅₀	2815 nM Compound: PL	Antiproliferative activity against human CMK cells after 72 hrs by MTT assay Antiproliferative activity against human CMK cells after 72 hrs by MTT assay	[PMID: 27505848]
CMK	IC₅₀	421.8 nM Compound: PL	Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs in presence of SAHA by MTT assay Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs in presence of SAHA by MTT assay	[PMID: 27505848]
CMK	IC₅₀	612.7 nM Compound: PL	Antiproliferative activity against human CMK cells after 72 hrs in presence of SAHA by MTT assay Antiproliferative activity against human CMK cells after 72 hrs in presence of SAHA by MTT assay	[PMID: 27505848]
DU-145	GI₅₀	7.1 μM Compound: 1; PL	Growth inhibition of human DU145 cells after 48 hrs by WST-1 assay Growth inhibition of human DU145 cells after 48 hrs by WST-1 assay	[PMID: 29807795]
HaCaT	IC₅₀	16 μM Compound: PL, piplartine	Cytotoxicity against human HaCaT cells assessed as reduction in cell viability after 24 hrs by MTT reduction assay Cytotoxicity against human HaCaT cells assessed as reduction in cell viability after 24 hrs by MTT reduction assay	[PMID: 25305718]
HaCaT	IC₅₀	3.03 μM Compound: 3	Cytotoxicity against human HaCaT assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HaCaT assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31400708]
HaCaT	EC₅₀	4.46 μM Compound: piperlongumine	Antiproliferative activity against human HaCaT cells after 72 hrs by MTT assay Antiproliferative activity against human HaCaT cells after 72 hrs by MTT assay	[PMID: 25826398]
HCT-116	EC₅₀	11.5 μM Compound: piperlongumine	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 25826398]
HCT-116	IC₅₀	6.04 μM Compound: PL	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 24937186]
HCT-116	IC₅₀	6.38 μM Compound: PL	Cytotoxicity against human HCT-116 incubated for 24 hrs by CCK-8 assay Cytotoxicity against human HCT-116 incubated for 24 hrs by CCK-8 assay	[PMID: 35696861]
HCT-116	IC₅₀	6.9 μM Compound: PL	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33026807]
HCT-116	IC₅₀	7.34 μM Compound: PL	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 28434764]
HCT-116	IC₅₀	8.13 μM Compound: 1	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 29424539]
HCT-116	IC₅₀	8.13 μM Compound: Piperlongumine	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 28686911]
HCT-116	IC₅₀	8.17 μM Compound: 1	Antiproliferative activity against human HCT116 cells after 72 hrs in presence of ligustrazine by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs in presence of ligustrazine by MTT assay	[PMID: 29424539]
HCT-116	IC₅₀	9.2 μM Compound: 1; PL	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 28159415]
HCT-8	IC₅₀	4.1 μM Compound: 1	Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay	[PMID: 29424539]
HCT-8	IC₅₀	4.1 μM Compound: Piperlongumine	Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay	[PMID: 28686911]
HeLa	IC₅₀	16.3 μM Compound: 8	Growth inhibition of human HeLa cells measured after 48 hrs by MTT assay Growth inhibition of human HeLa cells measured after 48 hrs by MTT assay	[PMID: 34669417]
Hep 3B2	IC₅₀	69.46 μM Compound: PL	Cytotoxicity against human Hep3B cells after 72 hrs by MTT assay Cytotoxicity against human Hep3B cells after 72 hrs by MTT assay	[PMID: 24937186]
HepG2	IC₅₀	6.8 μM Compound: 1	Antiproliferative activity against human HepG2 cells incubated for 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells incubated for 24 hrs by MTT assay	[PMID: 34806369]
HepG2	IC₅₀	6.8 μM Compound: PL	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33026807]
HepG2	IC₅₀	8.9 μM Compound: 1; PL	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 28159415]
HFF-1	EC₅₀	13.1 μM Compound: piperlongumine	Antiproliferative activity against HFF1 cells after 72 hrs by MTT assay Antiproliferative activity against HFF1 cells after 72 hrs by MTT assay	[PMID: 25826398]
HGC-27	IC₅₀	8.1 μM Compound: PL	Cytotoxicity against human HGC-27 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HGC-27 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33026807]
HGC-27	IC₅₀	8.2 μM Compound: 1	Antiproliferative activity against human HGC-27 cells incubated for 24 hrs by MTT assay Antiproliferative activity against human HGC-27 cells incubated for 24 hrs by MTT assay	[PMID: 34806369]
HL-60	IC₅₀	1128 nM Compound: PL	Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs in presence of SAHA by MTT assay Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs in presence of SAHA by MTT assay	[PMID: 27505848]
HL-60	IC₅₀	1778 nM Compound: PL	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 27505848]
HL-60	IC₅₀	2250 nM Compound: PL	Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs by MTT assay	[PMID: 27505848]
HL-60	IC₅₀	529.2 nM Compound: PL	Antiproliferative activity against human HL60 cells after 72 hrs in presence of SAHA by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs in presence of SAHA by MTT assay	[PMID: 27505848]
HT-1080	IC₅₀	3.43 μM Compound: PL	Cytotoxicity against human HT1080 cells assessed as cell viability after 72 hrs by resazurin reduction assay Cytotoxicity against human HT1080 cells assessed as cell viability after 72 hrs by resazurin reduction assay	[PMID: 26599530]
HT-29	ED₅₀	0.45 μg/mL Compound: 3	Cytotoxicity against human HT-29 cells after 6 days by MTT assay Cytotoxicity against human HT-29 cells after 6 days by MTT assay	[PMID: 2089124]
HT-29	IC₅₀	2.65 μM Compound: 1	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 29424539]
HT-29	IC₅₀	2.65 μM Compound: Piperlongumine	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 28686911]
HT-29	IC₅₀	5.49 μM Compound: PL	Cytotoxicity against human HT-29 cells assessed as cell viability after 72 hrs by resazurin reduction assay Cytotoxicity against human HT-29 cells assessed as cell viability after 72 hrs by resazurin reduction assay	[PMID: 26599530]
Jurkat	IC₅₀	1.4 μM Compound: 1; PL	Antiproliferative activity in human Jurkat cells assessed as cell viability after 48 hrs by alamarBlue assay Antiproliferative activity in human Jurkat cells assessed as cell viability after 48 hrs by alamarBlue assay	[PMID: 27689728]
Jurkat	IC₅₀	5 μM Compound: 1; PL	Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay	[PMID: 27689728]
K562	IC₅₀	5.05 μM Compound: 1	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay Antiproliferative activity against human K562 cells after 72 hrs by MTT assay	[PMID: 29424539]
K562	IC₅₀	5.09 μM Compound: 1	Antiproliferative activity against human K562 cells after 72 hrs in presence of ligustrazine by MTT assay Antiproliferative activity against human K562 cells after 72 hrs in presence of ligustrazine by MTT assay	[PMID: 29424539]
KB	IC₅₀	1.67 μM Compound: 1; PL	Antiproliferative activity against human KB cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human KB cells after 72 hrs by sulforhodamine B assay	[PMID: 32736231]
KB	ED₅₀	1.8 μg/mL Compound: 3	Cytotoxicity against human KB cells after 3 days by MTT assay Cytotoxicity against human KB cells after 3 days by MTT assay	[PMID: 2089124]
LNCaP	GI₅₀	> 10 μM Compound: 1; PL	Growth inhibition of human LNCAP cells after 24 to 48 hrs by WST-1 assay Growth inhibition of human LNCAP cells after 24 to 48 hrs by WST-1 assay	[PMID: 29807795]
LNCaP	GI₅₀	9.2 μM Compound: 1; PL	Growth inhibition of human LNCAP cells after 48 hrs by WST-1 assay Growth inhibition of human LNCAP cells after 48 hrs by WST-1 assay	[PMID: 29807795]
MCF-10A	EC₅₀	18.1 μM Compound: piperlongumine	Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay	[PMID: 25826398]
MCF7	IC₅₀	1.2 μM Compound: 1; PL	Antiproliferative activity in human MCF7 cells assessed as cell viability after 48 hrs by alamarBlue assay Antiproliferative activity in human MCF7 cells assessed as cell viability after 48 hrs by alamarBlue assay	[PMID: 27689728]
MCF7	IC₅₀	4.4 μM Compound: 1; PL	Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay	[PMID: 32736231]
MCF7	IC₅₀	6.14 μM Compound: PL	Cytotoxicity against human MCF7 cells assessed as cell viability after 72 hrs by resazurin reduction assay Cytotoxicity against human MCF7 cells assessed as cell viability after 72 hrs by resazurin reduction assay	[PMID: 26599530]
MCF7	IC₅₀	8 μM Compound: 1; PL	Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 27689728]
MDA-MB-231	IC₅₀	10.6 μM Compound: PL	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 28434764]
MDA-MB-231	IC₅₀	3.72 μM Compound: 1; PL	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay	[PMID: 32736231]
MDA-MB-231	IC₅₀	8.46 μM Compound: PL	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 24937186]
MOLM-13	IC₅₀	1838 nM Compound: PL	Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs by MTT assay Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs by MTT assay	[PMID: 27505848]
MOLM-13	IC₅₀	934.5 nM Compound: PL	Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs in presence of SAHA by MTT assay Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs in presence of SAHA by MTT assay	[PMID: 27505848]
MRC5	IC₅₀	35.04 μM Compound: PL	Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay	[PMID: 24937186]
MRC5	IC₅₀	37 μM Compound: 1; PL	Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay	[PMID: 28159415]
MV4-11	IC₅₀	1439 nM Compound: PL	Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay	[PMID: 27505848]
MV4-11	IC₅₀	289.1 nM Compound: PL	Antiproliferative activity against human MV4-11 cells after 72 hrs in presence of SAHA by MTT assay Antiproliferative activity against human MV4-11 cells after 72 hrs in presence of SAHA by MTT assay	[PMID: 27505848]
OCI-AML-3	IC₅₀	1109 nM Compound: PL	Antiproliferative activity against human OCI-AML3 cells after 72 hrs in presence of SAHA by MTT assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs in presence of SAHA by MTT assay	[PMID: 27505848]
OCI-AML-3	IC₅₀	1868 nM Compound: PL	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay	[PMID: 27505848]
P388	ED₅₀	0.9 μg/mL Compound: 3	Cytotoxicity against mouse P388 cells after 3 days by MTT assay Cytotoxicity against mouse P388 cells after 3 days by MTT assay	[PMID: 2089124]
PANC-1	IC₅₀	3.2 μM Compound: PL, piplartine	Cytotoxicity against human PANC1 cells assessed as reduction in cell viability after 24 hrs by MTT reduction assay Cytotoxicity against human PANC1 cells assessed as reduction in cell viability after 24 hrs by MTT reduction assay	[PMID: 25305718]
PC-3	GI₅₀	> 10 μM Compound: 1; PL	Growth inhibition of human PC3 cells after 24 to 48 hrs by WST-1 assay Growth inhibition of human PC3 cells after 24 to 48 hrs by WST-1 assay	[PMID: 29807795]
PC-3	GI₅₀	> 10 μM Compound: 1; PL	Growth inhibition of human PC3 cells after 48 hrs by WST-1 assay Growth inhibition of human PC3 cells after 48 hrs by WST-1 assay	[PMID: 29807795]
Platelet	IC₅₀	20.751 mM Compound: PL	Antiplatelet activity in rabbit plasma assessed as inhibition of arachidonic acid induced platelet aggregation by microplate reader analysis Antiplatelet activity in rabbit plasma assessed as inhibition of arachidonic acid induced platelet aggregation by microplate reader analysis	[PMID: 33930801]
Platelet	IC₅₀	6.71 mM Compound: PL	Antiplatelet activity in rabbit plasma assessed as inhibition of ADP induced platelet aggregation by microplate reader analysis Antiplatelet activity in rabbit plasma assessed as inhibition of ADP induced platelet aggregation by microplate reader analysis	[PMID: 33930801]
SAOS-2	IC₅₀	7.31 μM Compound: PL	Antiproliferative activity against human Saos2 cells after 72 hrs by MTT assay Antiproliferative activity against human Saos2 cells after 72 hrs by MTT assay	[PMID: 28434764]
SF-188	IC₅₀	3.9 μM Compound: PL	Cytotoxicity against human SF188 cells assessed as cell viability after 72 hrs by resazurin reduction assay Cytotoxicity against human SF188 cells assessed as cell viability after 72 hrs by resazurin reduction assay	[PMID: 26599530]
SH-SY5Y	IC₅₀	45.88 μM Compound: 3	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 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	[PMID: 31400708]
SH-SY5Y	IC₅₀	5.94 μM Compound: 3	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31400708]
SK-BR-3	IC₅₀	4.04 μM Compound: PL	Cytotoxicity against human SKBR3 cells assessed as cell viability after 72 hrs by resazurin reduction assay Cytotoxicity against human SKBR3 cells assessed as cell viability after 72 hrs by resazurin reduction assay	[PMID: 26599530]
SK-HEP1	IC₅₀	13.3 μM Compound: PL	Antiproliferative activity against human SKHEP1 cells after 72 hrs by MTT assay Antiproliferative activity against human SKHEP1 cells after 72 hrs by MTT assay	[PMID: 28434764]
SK-MEL-2	EC₅₀	4.39 μM Compound: piperlongumine	Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by MTT assay Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by MTT assay	[PMID: 25826398]
SW-620	IC₅₀	4.62 μM Compound: 1	Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay	[PMID: 29424539]
T98G	IC₅₀	4.92 μM Compound: PL	Cytotoxicity against human T98G cells assessed as cell viability after 72 hrs by resazurin reduction assay Cytotoxicity against human T98G cells assessed as cell viability after 72 hrs by resazurin reduction assay	[PMID: 26599530]
U2OS	IC₅₀	9.49 μM Compound: PL	Antiproliferative activity against human U2OS cells after 72 hrs by MTT assay Antiproliferative activity against human U2OS cells after 72 hrs by MTT assay	[PMID: 28434764]
U-87MG ATCC	IC₅₀	16.15 μM Compound: 1	Antiproliferative activity against human U87MG cells after 72 hrs in presence of ligustrazine by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs in presence of ligustrazine by MTT assay	[PMID: 29424539]
U-87MG ATCC	IC₅₀	17.34 μM Compound: 1	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay	[PMID: 29424539]
U-87MG ATCC	IC₅₀	7.18 μM Compound: 3	Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31400708]
U-937	IC₅₀	2174 nM Compound: PL	Antiproliferative activity against p53 null human U937 cells after 72 hrs by MTT assay Antiproliferative activity against p53 null human U937 cells after 72 hrs by MTT assay	[PMID: 27505848]
U-937	IC₅₀	767 nM Compound: PL	Antiproliferative activity against p53 null human U937 cells after 72 hrs in presence of SAHA by MTT assay Antiproliferative activity against p53 null human U937 cells after 72 hrs in presence of SAHA by MTT assay	[PMID: 27505848]
WI-38	IC₅₀	> 100 μM Compound: PL	Cytotoxicity against human W138 cells after 72 hrs by MTT assay Cytotoxicity against human W138 cells after 72 hrs by MTT assay	[PMID: 28434764]
WI-38	EC₅₀	20.3 μM Compound: PL	Senolytic activity against non-senescent human WI38 cells assessed as reduction in cell viability by propidium iodide staining based flow cytometry Senolytic activity against non-senescent human WI38 cells assessed as reduction in cell viability by propidium iodide staining based flow cytometry	[PMID: 29925484]
WI-38	IC₅₀	26.78 μM Compound: PL	Cytotoxicity against human WI38 cells after 72 hrs by MTT assay Cytotoxicity against human WI38 cells after 72 hrs by MTT assay	[PMID: 24937186]
WI-38	EC₅₀	8 μM Compound: PL	Senolytic activity against ionizing radiation induced human WI38 senescent cells assessed as reduction in cell viability by propidium iodide staining based flow cytometry Senolytic activity against ionizing radiation induced human WI38 senescent cells assessed as reduction in cell viability by propidium iodide staining based flow cytometry	[PMID: 29925484]
ZR-75-30	IC₅₀	5.86 μM Compound: PL	Cytotoxicity against human ZR75-30 cells after 72 hrs by MTT assay Cytotoxicity against human ZR75-30 cells after 72 hrs by MTT assay	[PMID: 24937186]

In Vitro

Piplartine (5, 10, and 15 μM) significantly decreases cell proliferation of 786-O, SKBR3, Panc1, A549, and L3.6pL cancer cells after treatment for 24 and 48 hours, induces apoptosis and ROS in these cell lines at 5 and 10 μM after 3 or 9 h of treatment^[1].
Piplartine (5 or 10 μM) induces cleaved PARP and downregulates Sp1, Sp3, Sp4, and Sp-regulated genes^[1].
Piplartine (20 μM) decreases the viability of cardiac fibroblasts (CFs). Piplartine (0-10 μM) suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Piperlongumine (30 mg/kg/day, i.p. for 3 weeks) exhibits potent anti-tumor effect in athymic nude mice bearing L3.6pL cells without body weight loss^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

317.34

Formula

C₁₇H₁₉NO₅

CAS No.

20069-09-4

Appearance

Solid

Color

White to yellow

SMILES

O=C1C=CCCN1C(/C=C/C2=CC(OC)=C(OC)C(OC)=C2)=O

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (315.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1512 mL	15.7560 mL	31.5119 mL
5 mM	0.6302 mL	3.1512 mL	6.3024 mL
10 mM	0.3151 mL	1.5756 mL	3.1512 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (249 KB) HNMR (258 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Karki K, et al. Piperlongumine Induces Reactive Oxygen Species (ROS)-Dependent Downregulation of Specificity Protein Transcription Factors. [Content Brief]

[2]. Wu X, e,t al. Piperlongumine inhibits angiotensin II-induced extracellular matrix expression in cardiac fibroblasts. J Cell Biochem. 2018 Dec;119(12):10358-10364 [Content Brief]

[3]. Yan Qin , et al. Pan-cancer analysis identifies migrasome-related genes as a potential immunotherapeutic target: A bulk omics research and single cell sequencing validation. Front Immunol. 2022 Nov 3;13:994828. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.1512 mL	15.7560 mL	31.5119 mL	78.7799 mL
	5 mM	0.6302 mL	3.1512 mL	6.3024 mL	15.7560 mL
	10 mM	0.3151 mL	1.5756 mL	3.1512 mL	7.8780 mL
	15 mM	0.2101 mL	1.0504 mL	2.1008 mL	5.2520 mL
	20 mM	0.1576 mL	0.7878 mL	1.5756 mL	3.9390 mL
	25 mM	0.1260 mL	0.6302 mL	1.2605 mL	3.1512 mL
	30 mM	0.1050 mL	0.5252 mL	1.0504 mL	2.6260 mL
	40 mM	0.0788 mL	0.3939 mL	0.7878 mL	1.9695 mL
	50 mM	0.0630 mL	0.3151 mL	0.6302 mL	1.5756 mL
	60 mM	0.0525 mL	0.2626 mL	0.5252 mL	1.3130 mL
	80 mM	0.0394 mL	0.1969 mL	0.3939 mL	0.9847 mL
	100 mM	0.0315 mL	0.1576 mL	0.3151 mL	0.7878 mL

Piperlongumine Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Piperlongumine20069-09-4PiplartineERKReactive Oxygen SpeciesAutophagyApoptosisBacterialFerroptosisExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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Piperlongumine (Synonyms: Piplartine)

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Complete Stock Solution Preparation Table

Piperlongumine Related Classifications

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