Lapachol

Name: Lapachol
Brand: MedChemExpress
SKU: HY-N6961
Rating: 5.0 (2 reviews)

Cat. No.: HY-N6961 Purity: 99.06%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

Lapachol Chemical Structure

CAS No. : 84-79-7

Size	Price	Stock	Quantity
5 mg	USD 32	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Lapachol:

Lapachol (Standard) Get quote

2 Publications Citing Use of MCE Lapachol

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Parasite Isoform Specific Products:

View All Isoforms

Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Plasmodium

Leishmania

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	GI₅₀	1.9 μM 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	IC₅₀	> 30 μM 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	CC₅₀	≥ 285 μM 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	EC₅₀	4.78 μM 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	8 μM Compound: 1, Lapachol	Growth inhibition of human A549 cells by MTT assay Growth inhibition of human A549 cells by MTT assay	[PMID: 24374273]
DU-145	IC₅₀	64.59 nM 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]
ECa-109 cell line	IC₅₀	12.56 μM 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 μM 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 μM 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 μM 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 μM 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 μM 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 μM 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]
HepG2	CC₅₀	≥ 285 μM 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 μM 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 μM 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 μM 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 μM 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]
K562	IC₅₀	> 10 μM 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]
LLC-PK1	CC₅₀	≥ 285 μM 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 μM Compound: 1, Lapachol	Growth inhibition of human LoVo cells by MTT assay Growth inhibition of human LoVo cells by MTT assay	[PMID: 24374273]
MCF7	IC₅₀	> 30 μM 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]
MCF7	EC₅₀	10.15 μM 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]
MDA-MB-231	IC₅₀	> 10 μM 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]
MDA-MB-231	IC₅₀	> 30 μM 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]
MRC5	CC₅₀	≥ 285 μM 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]
PBMC	IC₅₀	> 103.19 μM 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]
PBMC	IC₅₀	2.1 μM 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]
PC-3	EC₅₀	1.97 μM 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 μM Compound: 1, Lapachol	Growth inhibition of human PC3 cells by MTT assay Growth inhibition of human PC3 cells by MTT assay	[PMID: 24374273]
Peritoneal macrophage cell	CC₅₀	59.3 μM 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]
Raji	IC₅₀	311.4 μM 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]
SK-MEL-28	IC₅₀	8 μM 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 μM 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 μM 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 μM 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 μM 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 μM 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 μM 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 μM 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.

Molecular Weight

242.27

Formula

C₁₅H₁₄O₃

CAS No.

84-79-7

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Solvent & Solubility

In Vitro:

DMSO : 66.67 mg/mL (275.19 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
10 mM	0.4128 mL	2.0638 mL	4.1276 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.

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 (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.

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).

*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.

Purity & Documentation

Purity: 99.06%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (249 KB) HNMR (237 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Raphael S Peres, et al. Lapachol, a compound targeting pyrimidine metabolism, ameliorates experimental autoimmune arthritis. Arthritis Res Ther. 2017 Mar 7;19(1):47. [Content Brief]

[2]. Masayo Maeda, et al. Promotion or suppression of experimental metastasis of B16 melanoma cells after oral administration of lapachol. Toxicol Appl Pharmacol. 2008 Jun 1;229(2):232-8. [Content Brief]

[3]. Iasmin Aparecida Cunha Araújo, et al. Efficacy of lapachol on treatment of cutaneous and visceral leishmaniasis. Exp Parasitol. 2019 Apr:199:67-73. [Content Brief]

Complete Stock Solution Preparation Table

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

Lapachol 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:

Lapachol84-79-7Dihydroorotate DehydrogenaseDNA/RNA SynthesisParasiteDHODHnaphthoquinoneimmunosuppressivelymphocytespyrimidine synthesisvitamin Kantitumorneoplastic cellsanti-LeishmaniaInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Lapachol

Customer Review

Other Forms of Lapachol:

Lapachol Related Antibodies

2 Publications Citing Use of MCE Lapachol

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Parasite Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Lapachol Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Lapachol Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report