1. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Anti-infection
  2. Dihydroorotate Dehydrogenase DNA/RNA Synthesis Parasite
  3. Lapachol

Lapachol, a natural naphthoquinone, is an orally active, potent DHODH inhibitor. Lapachol has immunosuppressive activity on lymphocytes through its direct ability to block DHODH activity and inhibit pyrimidine synthesis. Lapachol is a vitamin K antagonist with antitumor activity and can inhibit DNA and RNA synthesis in neoplastic cells. Lapachol has anti-Leishmania activity.

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Lapachol

Lapachol Chemische Struktur

CAS. Nr. : 84-79-7

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Based on 3 publication(s) in Google Scholar

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Beschreibung

Lapachol, a natural naphthoquinone, is an orally active, potent DHODH inhibitor. Lapachol has immunosuppressive activity on lymphocytes through its direct ability to block DHODH activity and inhibit pyrimidine synthesis. Lapachol is a vitamin K antagonist with antitumor activity and can inhibit DNA and RNA synthesis in neoplastic cells. Lapachol has anti-Leishmania activity[1][2][3].

IC50 & Target

Plasmodium

 

Leishmania

 

Cellular Effect
Cell Line Type Value Description References
A2780 GI50
1.9 3
Compound: 3
Growth inhibition of human A2780 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human A2780 cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
A2780 GI50
1.9 3
Compound: 3
Growth inhibition of human A2780 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human A2780 cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
A2780 GI50
1.9 3
Compound: 3
Growth inhibition of human A2780 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human A2780 cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
A549 CC50
>= 285 3
Compound: 28
Cytotoxicity against human A549 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human A549 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
A549 CC50
>= 285 3
Compound: 28
Cytotoxicity against human A549 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human A549 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
A549 IC50
> 30 3
Compound: 3
Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
A549 EC50
4.78 3
Compound: 3
Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
A549 EC50
4.78 3
Compound: 3
Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
A549 CC50
≥ 285 3
Compound: 28
Cytotoxicity against human A549 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human A549 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
A549 IC50
8 3
Compound: 1, Lapachol
Growth inhibition of human A549 cells by MTT assay
Growth inhibition of human A549 cells by MTT assay
[PMID: 24374273]
A549 EC50
4.78 3
Compound: 3
Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human A549 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
A549 IC50
>30 3
Compound: 3
Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
A549 IC50
8 3
Compound: 1, Lapachol
Growth inhibition of human A549 cells by MTT assay
Growth inhibition of human A549 cells by MTT assay
[PMID: 24374273]
A549 IC50
8 3
Compound: 1, Lapachol
Growth inhibition of human A549 cells by MTT assay
Growth inhibition of human A549 cells by MTT assay
[PMID: 24374273]
A549 IC50
> 30 3
Compound: 3
Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
ECa-109 cell line IC50
12.56 3
Compound: Lapachol
Cytotoxicity against human ECA109 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay
Cytotoxicity against human ECA109 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay
[PMID: 27667553]
DU-145 IC50
64.59 1
Compound: 1
Anticancer activity against human DU145 cells after 72 hrs by XTT assay
Anticancer activity against human DU145 cells after 72 hrs by XTT assay
[PMID: 18829316]
C6 IC50
3.7 3
Compound: Lapachol
Antiproliferative activity against rat C6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS/PMS assay
Antiproliferative activity against rat C6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS/PMS assay
[PMID: 38458106]
ECa-109 cell line IC50
12.56 3
Compound: Lapachol
Cytotoxicity against human ECA109 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay
Cytotoxicity against human ECA109 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay
[PMID: 27667553]
HBL-100 GI50
7.8 3
Compound: 3
Growth inhibition of human HBL100 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HBL100 cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
HBL-100 GI50
7.8 3
Compound: 1
Growth inhibition of human HBL100 cells by SRB assay
Growth inhibition of human HBL100 cells by SRB assay
[PMID: 22560628]
HBL-100 GI50
7.8 3
Compound: 1
Growth inhibition of human HBL100 cells by SRB assay
Growth inhibition of human HBL100 cells by SRB assay
[PMID: 22560628]
HBL-100 GI50
7.8 3
Compound: 3
Growth inhibition of human HBL100 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HBL100 cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
HeLa GI50
2.3 3
Compound: 3
Growth inhibition of human HeLa cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HeLa cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
DU-145 IC50
64.59 1
Compound: 1
Anticancer activity against human DU145 cells after 72 hrs by XTT assay
Anticancer activity against human DU145 cells after 72 hrs by XTT assay
[PMID: 18829316]
HeLa GI50
2.3 3
Compound: 1
Growth inhibition of human HeLa cells by SRB assay
Growth inhibition of human HeLa cells by SRB assay
[PMID: 22560628]
HeLa GI50
2.3 3
Compound: 1
Growth inhibition of human HeLa cells by SRB assay
Growth inhibition of human HeLa cells by SRB assay
[PMID: 22560628]
HeLa GI50
2.3 3
Compound: 3
Growth inhibition of human HeLa cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HeLa cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
HeLa IC50
20.36 3
Compound: Lapachol
Cytotoxicity against human HeLa cells assessed as decrease in cell proliferation after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as decrease in cell proliferation after 48 hrs by MTT assay
[PMID: 27667553]
HBL-100 GI50
7.8 3
Compound: 1
Growth inhibition of human HBL100 cells by SRB assay
Growth inhibition of human HBL100 cells by SRB assay
[PMID: 22560628]
HeLa IC50
20.36 3
Compound: Lapachol
Cytotoxicity against human HeLa cells assessed as decrease in cell proliferation after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as decrease in cell proliferation after 48 hrs by MTT assay
[PMID: 27667553]
HepG2 CC50
>4130.7 3
Compound: 1
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 29324340]
HBL-100 GI50
7.8 3
Compound: 3
Growth inhibition of human HBL100 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HBL100 cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
HepG2 CC50
> 4130.7 3
Compound: 1
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 29324340]
HL-60 IC50
3.18 3
Compound: 1
Cytotoxicity against human promyelocytic leukemia HL60 cell line by MTT assay
Cytotoxicity against human promyelocytic leukemia HL60 cell line by MTT assay
[PMID: 17249647]
HepG2 CC50
>= 285 3
Compound: 28
Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
HepG2 CC50
≥ 285 3
Compound: 28
Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
HL-60 IC50
3.18 3
Compound: 1
Cytotoxicity against human promyelocytic leukemia HL60 cell line by MTT assay
Cytotoxicity against human promyelocytic leukemia HL60 cell line by MTT assay
[PMID: 17249647]
HT-29 EC50
2.84 3
Compound: Lapachol
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
[PMID: 24900447]
HL-60 IC50
3.18 3
Compound: 1
Cytotoxicity against human promyelocytic leukemia HL60 cell line by MTT assay
Cytotoxicity against human promyelocytic leukemia HL60 cell line by MTT assay
[PMID: 17249647]
Hs 683 IC50
11 3
Compound: 1, Lapachol
Growth inhibition of human Hs683 cells by MTT assay
Growth inhibition of human Hs683 cells by MTT assay
[PMID: 24374273]
Hs 683 IC50
11 3
Compound: 1, Lapachol
Growth inhibition of human Hs683 cells by MTT assay
Growth inhibition of human Hs683 cells by MTT assay
[PMID: 24374273]
HT-29 EC50
2.84 3
Compound: Lapachol
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
[PMID: 24900447]
HT-29 EC50
2.84 3
Compound: Lapachol
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
[PMID: 24900447]
HT-29 IC50
4.66 3
Compound: Lapachol
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
[PMID: 24900447]
HT-29 IC50
4.66 3
Compound: Lapachol
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
[PMID: 24900447]
HT-29 IC50
4.66 3
Compound: Lapachol
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
[PMID: 24900447]
HaCaT IC50
> 10 3
Compound: 1
Antiproliferative activity against human HaCaT cells
Antiproliferative activity against human HaCaT cells
[PMID: 10479319]
HeLa GI50
2.3 3
Compound: 1
Growth inhibition of human HeLa cells by SRB assay
Growth inhibition of human HeLa cells by SRB assay
[PMID: 22560628]
K562 IC50
>10 3
Compound: 1
Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
[PMID: 30003778]
K562 IC50
> 10 3
Compound: 1
Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
[PMID: 30003778]
HeLa GI50
2.3 3
Compound: 3
Growth inhibition of human HeLa cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human HeLa cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
LLC-PK1 CC50
≥ 285 3
Compound: 28
Cytotoxicity against human LLC-PK1 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human LLC-PK1 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
LoVo IC50
9 3
Compound: 1, Lapachol
Growth inhibition of human LoVo cells by MTT assay
Growth inhibition of human LoVo cells by MTT assay
[PMID: 24374273]
HeLa IC50
20.36 3
Compound: Lapachol
Cytotoxicity against human HeLa cells assessed as decrease in cell proliferation after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as decrease in cell proliferation after 48 hrs by MTT assay
[PMID: 27667553]
LLC-PK1 CC50
>= 285 3
Compound: 28
Cytotoxicity against human LLC-PK1 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human LLC-PK1 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
MCF7 IC50
> 30 3
Compound: 3
Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
HepG2 CC50
> 4130.7 3
Compound: 1
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 29324340]
LoVo IC50
9 3
Compound: 1, Lapachol
Growth inhibition of human LoVo cells by MTT assay
Growth inhibition of human LoVo cells by MTT assay
[PMID: 24374273]
MCF7 EC50
10.15 3
Compound: 3
Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
HepG2 CC50
>= 285 3
Compound: 28
Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
MCF7 EC50
10.15 3
Compound: 3
Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
Hs 683 IC50
11 3
Compound: 1, Lapachol
Growth inhibition of human Hs683 cells by MTT assay
Growth inhibition of human Hs683 cells by MTT assay
[PMID: 24374273]
MDA-MB-231 IC50
> 10 3
Compound: 1
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
[PMID: 30003778]
DU-145 IC50
64.59 1
Compound: 1
Anticancer activity against human DU145 cells after 72 hrs by XTT assay
Anticancer activity against human DU145 cells after 72 hrs by XTT assay
[PMID: 18829316]
K562 IC50
> 10 3
Compound: 1
Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
[PMID: 30003778]
MDA-MB-231 IC50
> 30 3
Compound: 3
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
MCF7 IC50
>30 3
Compound: 3
Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
KB ED50
4.4 6
Compound: 21 (lapachol)
Evaluated for cytotoxicity in the KB cell culture assay
Evaluated for cytotoxicity in the KB cell culture assay
[PMID: 3669007]
MRC5 CC50
≥ 285 3
Compound: 28
Cytotoxicity against human MRC5 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human MRC5 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
MDA-MB-231 IC50
>10 3
Compound: 1
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
[PMID: 30003778]
PBMC IC50
> 103.19 3
Compound: 1
Cytotoxicity against human PBMC after 72 hrs by Alamar blue assay
Cytotoxicity against human PBMC after 72 hrs by Alamar blue assay
[PMID: 21820768]
KB ED50
4.4 6
Compound: 9
Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
[PMID: 7153777]
MDA-MB-231 IC50
>30 3
Compound: 3
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
LLC-PK1 CC50
>= 285 3
Compound: 28
Cytotoxicity against human LLC-PK1 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human LLC-PK1 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
PBMC IC50
2.1 3
Compound: 1, Lapachol
Cytotoxicity against human PBMC after 72 hrs by alamar blue assay
Cytotoxicity against human PBMC after 72 hrs by alamar blue assay
[PMID: 20378360]
LoVo IC50
9 3
Compound: 1, Lapachol
Growth inhibition of human LoVo cells by MTT assay
Growth inhibition of human LoVo cells by MTT assay
[PMID: 24374273]
MRC5 CC50
>= 285 3
Compound: 28
Cytotoxicity against human MRC5 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human MRC5 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
PC-3 EC50
1.97 3
Compound: 3
Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
PC-3 IC50
4 3
Compound: 1, Lapachol
Growth inhibition of human PC3 cells by MTT assay
Growth inhibition of human PC3 cells by MTT assay
[PMID: 24374273]
MCF7 EC50
10.15 3
Compound: 3
Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
PBMC IC50
2.1 3
Compound: 1, Lapachol
Cytotoxicity against human PBMC after 72 hrs by alamar blue assay
Cytotoxicity against human PBMC after 72 hrs by alamar blue assay
[PMID: 20378360]
MCF7 IC50
> 30 3
Compound: 3
Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
Peritoneal macrophage cell CC50
59.3 3
Compound: 10, Lapachol
Cytotoxicity against Swiss mouse peritoneal macrophages after 24 hrs by MTT assay
Cytotoxicity against Swiss mouse peritoneal macrophages after 24 hrs by MTT assay
[PMID: 23535320]
MDA-MB-231 IC50
> 10 3
Compound: 1
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
[PMID: 30003778]
PBMC IC50
>103.19 3
Compound: 1
Cytotoxicity against human PBMC after 72 hrs by Alamar blue assay
Cytotoxicity against human PBMC after 72 hrs by Alamar blue assay
[PMID: 21820768]
Raji IC50
311.4 3
Compound: 3
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced EBV-early antigen activation in human Raji cells after 48 hrs by immunofluorescence technique
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced EBV-early antigen activation in human Raji cells after 48 hrs by immunofluorescence technique
[PMID: 19674905]
PC-3 EC50
1.97 3
Compound: 3
Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
MDA-MB-231 IC50
> 30 3
Compound: 3
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay
[PMID: 32044231]
SK-MEL-28 IC50
8 3
Compound: 1, Lapachol
Growth inhibition of human SK-MEL-28 cells by MTT assay
Growth inhibition of human SK-MEL-28 cells by MTT assay
[PMID: 24374273]
MRC5 CC50
>= 285 3
Compound: 28
Cytotoxicity against human MRC5 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human MRC5 cells incubated for 24 hrs by MTT assay
[PMID: 33333397]
PC-3 IC50
4 3
Compound: 1, Lapachol
Growth inhibition of human PC3 cells by MTT assay
Growth inhibition of human PC3 cells by MTT assay
[PMID: 24374273]
SW1573 GI50
34 3
Compound: 1
Growth inhibition of human SW1573 cells by SRB assay
Growth inhibition of human SW1573 cells by SRB assay
[PMID: 22560628]
Peritoneal macrophage cell CC50
59.3 3
Compound: 10, Lapachol
Cytotoxicity against Swiss mouse peritoneal macrophages after 24 hrs by MTT assay
Cytotoxicity against Swiss mouse peritoneal macrophages after 24 hrs by MTT assay
[PMID: 23535320]
P388 IC50
0.2 6
Compound: 2
Cytotoxicity against mouse P388 cells
Cytotoxicity against mouse P388 cells
[PMID: 1791483]
SW1573 GI50
34 3
Compound: 3
Growth inhibition of human SW1573 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SW1573 cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
PBMC IC50
2.1 3
Compound: 1, Lapachol
Cytotoxicity against human PBMC after 72 hrs by alamar blue assay
Cytotoxicity against human PBMC after 72 hrs by alamar blue assay
[PMID: 20378360]
Raji IC50
311.4 3
Compound: 3
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced EBV-early antigen activation in human Raji cells after 48 hrs by immunofluorescence technique
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced EBV-early antigen activation in human Raji cells after 48 hrs by immunofluorescence technique
[PMID: 19674905]
T47D GI50
76 3
Compound: 3
Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
U2OS EC50
47.9 3
Compound: Lapachol
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
[PMID: 24900447]
PBMC IC50
> 103.19 3
Compound: 1
Cytotoxicity against human PBMC after 72 hrs by Alamar blue assay
Cytotoxicity against human PBMC after 72 hrs by Alamar blue assay
[PMID: 21820768]
Raji IC50
311.4 3
Compound: Lapachol
Inhibition of TPA-induced EBV-EA activation in Raji cells
Inhibition of TPA-induced EBV-EA activation in Raji cells
[PMID: 17950604]
SK-MEL-28 IC50
8 3
Compound: 1, Lapachol
Growth inhibition of human SK-MEL-28 cells by MTT assay
Growth inhibition of human SK-MEL-28 cells by MTT assay
[PMID: 24374273]
U-373MG ATCC IC50
8 3
Compound: 1, Lapachol
Growth inhibition of human U373 cells by MTT assay
Growth inhibition of human U373 cells by MTT assay
[PMID: 24374273]
PC-3 EC50
1.97 3
Compound: 3
Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue exclusion assay
Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue exclusion assay
[PMID: 19674905]
SW1573 GI50
34 3
Compound: 3
Growth inhibition of human SW1573 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SW1573 cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
PC-3 IC50
4 3
Compound: 1, Lapachol
Growth inhibition of human PC3 cells by MTT assay
Growth inhibition of human PC3 cells by MTT assay
[PMID: 24374273]
WiDr GI50
36 3
Compound: 1
Growth inhibition of human WiDr cells by SRB assay
Growth inhibition of human WiDr cells by SRB assay
[PMID: 22560628]
Peritoneal macrophage cell CC50
59.3 3
Compound: 10, Lapachol
Cytotoxicity against Swiss mouse peritoneal macrophages after 24 hrs by MTT assay
Cytotoxicity against Swiss mouse peritoneal macrophages after 24 hrs by MTT assay
[PMID: 23535320]
SW1573 GI50
34 3
Compound: 1
Growth inhibition of human SW1573 cells by SRB assay
Growth inhibition of human SW1573 cells by SRB assay
[PMID: 22560628]
WiDr GI50
36 3
Compound: 3
Growth inhibition of human WiDr cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human WiDr cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
T47D GI50
76 3
Compound: 3
Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
U2OS EC50
47.9 3
Compound: Lapachol
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
[PMID: 24900447]
U-373MG ATCC IC50
8 3
Compound: 1, Lapachol
Growth inhibition of human U373 cells by MTT assay
Growth inhibition of human U373 cells by MTT assay
[PMID: 24374273]
WiDr GI50
36 3
Compound: 3
Growth inhibition of human WiDr cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human WiDr cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
WiDr GI50
36 3
Compound: 1
Growth inhibition of human WiDr cells by SRB assay
Growth inhibition of human WiDr cells by SRB assay
[PMID: 22560628]
Raji IC50
311.4 3
Compound: 3
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced EBV-early antigen activation in human Raji cells after 48 hrs by immunofluorescence technique
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced EBV-early antigen activation in human Raji cells after 48 hrs by immunofluorescence technique
[PMID: 19674905]
Raji IC50
311.4 3
Compound: Lapachol
Inhibition of TPA-induced EBV-EA activation in Raji cells
Inhibition of TPA-induced EBV-EA activation in Raji cells
[PMID: 17950604]
SK-MEL-28 IC50
8 3
Compound: 1, Lapachol
Growth inhibition of human SK-MEL-28 cells by MTT assay
Growth inhibition of human SK-MEL-28 cells by MTT assay
[PMID: 24374273]
SW1573 GI50
34 3
Compound: 1
Growth inhibition of human SW1573 cells by SRB assay
Growth inhibition of human SW1573 cells by SRB assay
[PMID: 22560628]
SW1573 GI50
34 3
Compound: 3
Growth inhibition of human SW1573 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human SW1573 cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
T47D GI50
76 3
Compound: 3
Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human T47D cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
U-373MG ATCC IC50
8 3
Compound: 1, Lapachol
Growth inhibition of human U373 cells by MTT assay
Growth inhibition of human U373 cells by MTT assay
[PMID: 24374273]
U2OS EC50
47.9 3
Compound: Lapachol
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
[PMID: 24900447]
WiDr GI50
36 3
Compound: 1
Growth inhibition of human WiDr cells by SRB assay
Growth inhibition of human WiDr cells by SRB assay
[PMID: 22560628]
WiDr GI50
36 3
Compound: 3
Growth inhibition of human WiDr cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human WiDr cells after 48 hrs by sulforhodamine B assay
[PMID: 20304655]
In Vitro

Lapachol (10, 30, 100 μM; 4 days) inhibits lymphocyte proliferation through inhibition of pyrimidine biosynthesis[1].

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

Cell Proliferation Assay[1]

Cell Line: Murine CD4 T cells
Concentration: 10, 30, 100 μM
Incubation Time: 4 days
Result: Inhibited the proliferation of murine CD4 T cells in a dose-dependent manner.
In Vivo

Lapachol (3 mg/kg and 10 mg/kg; orally; once a day for 4 weeks) reduces the severity of experimental arthritis in CIA mice models[1].
Lapachol (10 mg/kg; orally; once a day over 9 days) exhibits a remarkable reduction in leucocyte infiltration into the knee joint 6 h after mBSA challenge in male C57BL/6 mice (6 weeks old) with antigen-induced arthritis (AIA)[1].

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

Animal Model: Male DBA1/J mice (10-12 weeks old) with collagen-induced arthritis (CIA) models[1]
Dosage: 3 mg/kg and 10 mg/kg
Administration: Orally; once a day for 4 weeks
Result: Markedly attenuated the severity of arthritis in CIA mice at both doses.
Markedly reduced all histopathological features of arthritis severity.
Molekulargewicht

242.27

Formel

C15H14O3

CAS. Nr.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C(CC=C(C)C)=C1O)C2=CC=CC=C2C1=O

Structure Classification
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 50 mg/mL (206.38 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 4.1276 mL 20.6381 mL 41.2763 mL
5 mM 0.8255 mL 4.1276 mL 8.2553 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (10.32 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.32 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 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)

g

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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.
Reinheit & Dokumentation

Purity: 99.49%

Verweise

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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.1276 mL 20.6381 mL 41.2763 mL 103.1907 mL
5 mM 0.8255 mL 4.1276 mL 8.2553 mL 20.6381 mL
10 mM 0.4128 mL 2.0638 mL 4.1276 mL 10.3191 mL
15 mM 0.2752 mL 1.3759 mL 2.7518 mL 6.8794 mL
20 mM 0.2064 mL 1.0319 mL 2.0638 mL 5.1595 mL
25 mM 0.1651 mL 0.8255 mL 1.6511 mL 4.1276 mL
30 mM 0.1376 mL 0.6879 mL 1.3759 mL 3.4397 mL
40 mM 0.1032 mL 0.5160 mL 1.0319 mL 2.5798 mL
50 mM 0.0826 mL 0.4128 mL 0.8255 mL 2.0638 mL
60 mM 0.0688 mL 0.3440 mL 0.6879 mL 1.7198 mL
80 mM 0.0516 mL 0.2580 mL 0.5160 mL 1.2899 mL
100 mM 0.0413 mL 0.2064 mL 0.4128 mL 1.0319 mL
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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.

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