Cat. No.: HY-13555

β-Lapachone

(Synonyms: ARQ-501; NSC-26326)

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.

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

Purity: 99.93%
CAS No.: 4707-32-8
Formula: C₁₅H₁₄O₃
Molecular Weight:242.27

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

β-Lapachone Chemical Structure

CAS No.: 4707-32-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (14)
Solvent & Solubility
- In Vitro
- In Vivo
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Biological Activity

Description

β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.

IC₅₀ & Target^[1]

Topoisomerase I

All Indoleamine 2,3-Dioxygenase (IDO) Isoforms :

All Topoisomerase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
1A9	IC₅₀	>0.8 μM Compound: 13	Cytotoxicity against paclitaxel-resistant human 1A9 cells after 3 days by SRB assay Cytotoxicity against paclitaxel-resistant human 1A9 cells after 3 days by SRB assay	[PMID: 15217280]
1A9	IC₅₀	0.8 μM Compound: 13	Cytotoxicity against human 1A9 cells after 3 days by SRB assay Cytotoxicity against human 1A9 cells after 3 days by SRB assay	[PMID: 15217280]
A2780	GI₅₀	1.1 μM Compound: 5	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	2.09 μM Compound: 30	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	4.21 μM Compound: 4	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	GI₅₀	0.8 μM Compound: beta-Lapachone	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 22819765]
A549	GI₅₀	3.32 μM Compound: Beta-lap	Cytotoxicity against human A549 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay	[PMID: 32464425]
A549	GI₅₀	6 μM Compound: Beta-lap	Cytotoxicity against human A549 cells assessed as reduction in cell growth pretreated for 1 hr with NQO1 inhibitor, dicoumarol followed by incubation with compound for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell growth pretreated for 1 hr with NQO1 inhibitor, dicoumarol followed by incubation with compound for 48 hrs by MTT assay	[PMID: 32464425]
A549	GI₅₀	6.19 μM Compound: Beta-lap	Cytotoxicity against human A549 cells assessed as reduction in cell growth pretreated for 1 hr with ROS scavenger, N-acetyl cysteine followed by incubation with compound for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell growth pretreated for 1 hr with ROS scavenger, N-acetyl cysteine followed by incubation with compound for 48 hrs by MTT assay	[PMID: 32464425]
A549	IC₅₀	>10 μM Compound: Beta-lapachone	Activation of NQO1 in human A549 cells assessed as decrease in cell survival incubated for 2 hrs measured after 7 days in presence of NQO1 inhibitor dicoumarol by Hoechst 33258 staining based assay Activation of NQO1 in human A549 cells assessed as decrease in cell survival incubated for 2 hrs measured after 7 days in presence of NQO1 inhibitor dicoumarol by Hoechst 33258 staining based assay	[PMID: 27341379]
A549	IC₅₀	0.8 μM Compound: Beta-Lapachone	Antiproliferative activity against apoptosis resistant human A549 cells after 72 hrs by MTT assay Antiproliferative activity against apoptosis resistant human A549 cells after 72 hrs by MTT assay	[PMID: 26883150]
A549	IC₅₀	1.5 μM Compound: 13	Cytotoxicity against human A549 cells after 3 days by SRB assay Cytotoxicity against human A549 cells after 3 days by SRB assay	[PMID: 15217280]
A549	IC₅₀	1.96 μM Compound: 5	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	1.96 μM Compound: 3	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by WST-8 method Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by WST-8 method	[PMID: 37343498]
A549	IC₅₀	16 μM Compound: Beta-lap	Cytotoxicity against human DPP-resistant A549 cells overexpressing NQO1 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human DPP-resistant A549 cells overexpressing NQO1 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33984806]
A549	IC₅₀	25 μM Compound: 1, beta-Lap	Cytotoxicity against human A549 cells after 72 hrs by MTT assay in presence of NQO1 inhibitor dicoumarol Cytotoxicity against human A549 cells after 72 hrs by MTT assay in presence of NQO1 inhibitor dicoumarol	[PMID: 25677663]
A549	IC₅₀	29 μM Compound: Beta-lap	Cytotoxicity against NQO1-deficient human A549 cells assessed as reduction in cell viability pretreated with DIC followed by compound addition and incubated for 72 hrs by MTT assay Cytotoxicity against NQO1-deficient human A549 cells assessed as reduction in cell viability pretreated with DIC followed by compound addition and incubated for 72 hrs by MTT assay	[PMID: 33984806]
A549	IC₅₀	3 μM Compound: Beta-lap	Substrate activity at NQO1 in human A549 cells assessed as NQO1-mediated two-electron reduction of compound by measuring cell growth inhibition treated for 24 hrs measured after 72 hrs by MTT assay Substrate activity at NQO1 in human A549 cells assessed as NQO1-mediated two-electron reduction of compound by measuring cell growth inhibition treated for 24 hrs measured after 72 hrs by MTT assay	[PMID: 28214631]
A549	IC₅₀	3.1 μM Compound: Beta-lap	Cytotoxicity against human A549 cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30508483]
A549	IC₅₀	3.32 μM Compound: Beta-lap	Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay	[PMID: 32682198]
A549	IC₅₀	3.4 μM Compound: Beta-lapachone	Activation of NQO1 in human A549 cells assessed as decrease in cell survival incubated for 2 hrs measured after 7 days by Hoechst 33258 staining based assay Activation of NQO1 in human A549 cells assessed as decrease in cell survival incubated for 2 hrs measured after 7 days by Hoechst 33258 staining based assay	[PMID: 27341379]
A549	IC₅₀	3.7 μM Compound: 1; beta-lap	Cytotoxicity against human A549 cells expressing NQO1 after 2 hrs by MTT assay Cytotoxicity against human A549 cells expressing NQO1 after 2 hrs by MTT assay	[PMID: 26803578]
A549	IC₅₀	3.7 μM Compound: 25	Antiproliferative activity against NQO1-positive human A549 cells Antiproliferative activity against NQO1-positive human A549 cells	[PMID: 35033884]
A549	IC₅₀	5.7 μM Compound: beta-lap	Cytotoxicity against NQO-1 rich human A549 cells assessed as inhibition of cell viability after 2 hrs by MTT assay Cytotoxicity against NQO-1 rich human A549 cells assessed as inhibition of cell viability after 2 hrs by MTT assay	[PMID: 24874653]
A549	IC₅₀	5.7 μM Compound: Beta-lap	Cytotoxicity against human A549 cells overexpressing NQO1 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells overexpressing NQO1 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33984806]
A549	IC₅₀	6 μM Compound: Beta-lap	Antiproliferative activity against human A549 cells measured after 48 hrs in presence of NQO1 inhibitor dicoumarol by MTT assay Antiproliferative activity against human A549 cells measured after 48 hrs in presence of NQO1 inhibitor dicoumarol by MTT assay	[PMID: 32682198]
A549	IC₅₀	7 μM Compound: 1, beta-Lap	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25677663]
A549/TR	IC₅₀	1.9 μM Compound: Beta-lap	Cytotoxicity against human A549/TR cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549/TR cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30508483]
A549/TR	IC₅₀	11 μM Compound: Beta-lap	Cytotoxicity against human A549/Taxol cells overexpressing NQO1 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A549/Taxol cells overexpressing NQO1 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33984806]
B16-F10	IC₅₀	0.3 μM Compound: Beta-Lapachone	Antiproliferative activity against apoptosis sensitive mouse B16F10 cells after 72 hrs by MTT assay Antiproliferative activity against apoptosis sensitive mouse B16F10 cells after 72 hrs by MTT assay	[PMID: 26883150]
BT-549	GI₅₀	11.4 μM Compound: 10	Antiproliferative activity against human BT-549 cells measured after 72 hrs by SRB assay Antiproliferative activity against human BT-549 cells measured after 72 hrs by SRB assay	[PMID: 35687347]
CAKI-1	IC₅₀	>5 μM Compound: 13	Cytotoxicity against human Caki1 cells after 3 days by SRB assay Cytotoxicity against human Caki1 cells after 3 days by SRB assay	[PMID: 15217280]
CAL-51	GI₅₀	8.3 μM Compound: 10	Antiproliferative activity against human CAL-51 cells measured after 72 hrs by SRB assay Antiproliferative activity against human CAL-51 cells measured after 72 hrs by SRB assay	[PMID: 35687347]
CCRF-CEM	GI₅₀	1.41 μM Compound: 1 (beta-Lapachone)	Cytotoxicity against leukemia CCRF-CEM cell lines Cytotoxicity against leukemia CCRF-CEM cell lines	[PMID: 11448231]
COLO 205	GI₅₀	1.78 μM Compound: 1 (beta-Lapachone)	Cytotoxicity against colon COKI 205 cell lines Cytotoxicity against colon COKI 205 cell lines	[PMID: 11448231]
DU-145	GI₅₀	1.74 μM Compound: 1 (beta-Lapachone)	Cytotoxicity against prostate DU-145 cell lines Cytotoxicity against prostate DU-145 cell lines	[PMID: 11448231]
DU-145	IC₅₀	7.4 nM Compound: 10	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]
Erythrocyte	EC₅₀	>200 μg/mL Compound: 2b, nor-beta-lapachone	Toxicity assessed as hemolytic activity against mouse erythrocyte Toxicity assessed as hemolytic activity against mouse erythrocyte	[PMID: 17827021]
Erythrocyte	EC₅₀	>50 μg/mL Compound: 1	Toxicity in mouse erythrocytes assessed as hemolytic activity after 30 mins by spectrophotometry Toxicity in mouse erythrocytes assessed as hemolytic activity after 30 mins by spectrophotometry	[PMID: 19947600]
HaCaT	IC₅₀	0.7 μM Compound: 4	Antiproliferative activity against human HaCaT cells Antiproliferative activity against human HaCaT cells	[PMID: 10479319]
HaCaT	IC₅₀	0.9 μM Compound: beta-lapachone	Antihyperproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy Antihyperproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy	[PMID: 22845014]
HaCaT	IC₅₀	0.9 μM Compound: beta-lapachone	Antihyperproliferative activity against human HaCaT cells assessed as inhibition of cell growth after 48 hrs by phase contrast microscopy Antihyperproliferative activity against human HaCaT cells assessed as inhibition of cell growth after 48 hrs by phase contrast microscopy	[PMID: 24964246]
HaCaT	IC₅₀	0.9 μM Compound: beta-lapachone	Antihyperproliferative activity against human HaCaT cells after 48 hrs by MTT assay Antihyperproliferative activity against human HaCaT cells after 48 hrs by MTT assay	[PMID: 28410493]
HBL1	GI₅₀	3.3 μM Compound: beta-Lapachone	Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay	[PMID: 38349664]
HBL-100	GI₅₀	0.38 μM Compound: 1b, ARQ 501, beta-lapachone	Growth inhibition of human HBL100 cells by SRB assay Growth inhibition of human HBL100 cells by SRB assay	[PMID: 22560628]
HBL-100	GI₅₀	0.69 μM Compound: 5	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]
HCC1954	GI₅₀	31.8 μM Compound: 10	Antiproliferative activity against human HCC1954 cells measured after 72 hrs by SRB assay Antiproliferative activity against human HCC1954 cells measured after 72 hrs by SRB assay	[PMID: 35687347]
HCT-116	GI₅₀	12.9 μM Compound: 10	Antiproliferative activity against human HCT-116 cells measured after 72 hrs by SRB assay Antiproliferative activity against human HCT-116 cells measured after 72 hrs by SRB assay	[PMID: 35687347]
HCT-116	IC₅₀	0.87 μM Compound: beta-lap	Cytotoxicity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
HCT-116	IC₅₀	0.87 μM Compound: Beta-lapachone	Cytotoxicity against human HCT116 cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27341379]
HCT-116	IC₅₀	0.97 μM Compound: beta-Lapachone	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	10.1039/C4MD00371C
HCT-8	IC₅₀	0.2 μg/mL Compound: 2b, nor-beta-lapachone	Cytotoxicity against human HCT8 cells after 72 hrs by MTT assay Cytotoxicity against human HCT8 cells after 72 hrs by MTT assay	[PMID: 17827021]
HCT-8	IC₅₀	0.83 μM Compound: 1	Cytotoxicity against human HCT8 cells after 72 hrs by MTT assay Cytotoxicity against human HCT8 cells after 72 hrs by MTT assay	[PMID: 19947600]
HCT-8	IC₅₀	0.83 μM Compound: b-lapachone	Cytotoxicity against human HCT8 cells after 72 hrs by MTT assay Cytotoxicity against human HCT8 cells after 72 hrs by MTT assay	[PMID: 21115213]
HCT-8	IC₅₀	0.95 μM Compound: beta-lap	Cytotoxicity against human HCT8 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human HCT8 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
HEK293	IC₅₀	25.31 μM Compound: 3b	Antiproliferative activity against HEK293 cells after 48 hrs by SRB assay Antiproliferative activity against HEK293 cells after 48 hrs by SRB assay	[PMID: 28094224]
HeLa	GI₅₀	0.81 μM Compound: 5	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	GI₅₀	1 μM Compound: 1b, ARQ 501, beta-lapachone	Growth inhibition of human HeLa cells by SRB assay Growth inhibition of human HeLa cells by SRB assay	[PMID: 22560628]
HeLa	GI₅₀	4.6 μM Compound: beta-Lapachone	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 22819765]
HeLa	IC₅₀	1 μM Compound: 31	Inhibition of IDO1 in human IFN-gamma induced HeLa cells assessed as reduction in L-kynurenine formation incubated for 5 hrs Inhibition of IDO1 in human IFN-gamma induced HeLa cells assessed as reduction in L-kynurenine formation incubated for 5 hrs	[PMID: 32055299]
HeLa	IC₅₀	1 μM Compound: beta-Lapachone	Inhibition of IDO1 in IFNgamma-induced human HeLa cells incubated for 5 hrs by Ehrlich's reagent based assay Inhibition of IDO1 in IFNgamma-induced human HeLa cells incubated for 5 hrs by Ehrlich's reagent based assay	[PMID: 31525930]
HepG2	CC₅₀	2.09 μM Compound: 30	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	GI₅₀	2.83 μM Compound: Beta-lap	Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay	[PMID: 32464425]
HepG2	GI₅₀	6.21 μM Compound: Beta-lap	Cytotoxicity against human HepG2 cells assessed as reduction in cell growth pretreated for 1 hr with ROS scavenger, N-acetyl cysteine followed by incubation with compound for 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell growth pretreated for 1 hr with ROS scavenger, N-acetyl cysteine followed by incubation with compound for 48 hrs by MTT assay	[PMID: 32464425]
HepG2	GI₅₀	6.3 μM Compound: Beta-lap	Cytotoxicity against human HepG2 cells assessed as reduction in cell growth pretreated for 1 hr with NQO1 inhibitor, dicoumarol followed by incubation with compound for 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell growth pretreated for 1 hr with NQO1 inhibitor, dicoumarol followed by incubation with compound for 48 hrs by MTT assay	[PMID: 32464425]
HepG2	IC₅₀	2.83 μM Compound: Beta-lap	Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay	[PMID: 32682198]
HL-60	IC₅₀	0.27 μM Compound: 15	Cytotoxicity against human promyelocytic leukemia HL60 cell line by MTT assay Cytotoxicity against human promyelocytic leukemia HL60 cell line by MTT assay	[PMID: 17249647]
HL-60	IC₅₀	0.4 μg/mL Compound: 2b, nor-beta-lapachone	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 17827021]
HL-60	IC₅₀	1.57 μM Compound: beta-lap	Cytotoxicity against human HL60 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human HL60 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
HL-60	IC₅₀	1.57 μM Compound: Beta-lapachone	Cytotoxicity against NQO1-deficient human HL60 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against NQO1-deficient human HL60 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27341379]
HL-60	IC₅₀	1.65 μM Compound: 1	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 19947600]
HL-60	IC₅₀	1.65 μM Compound: beta-Lapachone	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	10.1039/C4MD00371C
HL-60	IC₅₀	1.65 μM Compound: b-lapachone	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 21115213]
HOS	IC₅₀	1.4 μM Compound: 13	Cytotoxicity against human HOS cells after 3 days by SRB assay Cytotoxicity against human HOS cells after 3 days by SRB assay	[PMID: 15217280]
Hs 683	GI₅₀	0.4 μM Compound: beta-Lapachone	Antiproliferative activity against human Hs683 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human Hs683 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 22819765]
Hs 683	IC₅₀	0.4 μM Compound: Beta-Lapachone	Antiproliferative activity against apoptosis sensitive human Hs683 cells after 72 hrs by MTT assay Antiproliferative activity against apoptosis sensitive human Hs683 cells after 72 hrs by MTT assay	[PMID: 26883150]
J774.A1	IC₅₀	>200 μg/mL Compound: 1a; beta-lap	Cytotoxicity against mouse J774.A1 cells measured after 24 hrs by resazurin based assay Cytotoxicity against mouse J774.A1 cells measured after 24 hrs by resazurin based assay	[PMID: 31378595]
Jurkat	GI₅₀	6.1 μM Compound: beta-Lapachone	Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 22819765]
Jurkat	IC₅₀	1.9 μM Compound: 4a	Inhibition of MALT1 in human Jurkat cell lysate preincubated for 2 hrs followed by addition of 25 uM Ac-LRSR-AMC substrate for 3 hrs by fluorescence based assay Inhibition of MALT1 in human Jurkat cell lysate preincubated for 2 hrs followed by addition of 25 uM Ac-LRSR-AMC substrate for 3 hrs by fluorescence based assay	[PMID: 26496175]
K562	GI₅₀	41 μM Compound: 10	Antiproliferative activity against human K562 cells measured after 72 hrs by SRB assay Antiproliferative activity against human K562 cells measured after 72 hrs by SRB assay	[PMID: 35687347]
K562	IC₅₀	1.6 μM Compound: 3	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	4 μM Compound: beta-Lapachone	Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay	[PMID: 24775915]
KB	IC₅₀	1 μM Compound: 13	Cytotoxicity against camptothecin-resistant human KB cells after 3 days by SRB assay Cytotoxicity against camptothecin-resistant human KB cells after 3 days by SRB assay	[PMID: 15217280]
KB	IC₅₀	1.2 μM Compound: 13	Cytotoxicity against human KB cells after 3 days by SRB assay Cytotoxicity against human KB cells after 3 days by SRB assay	[PMID: 15217280]
KB	IC₅₀	1.8 μM Compound: 13	Cytotoxicity against etoposide-resistant human KB cells after 3 days by SRB assay Cytotoxicity against etoposide-resistant human KB cells after 3 days by SRB assay	[PMID: 15217280]
L02	GI₅₀	4.54 μM Compound: Beta-lap	Cytotoxicity against human L02 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay	[PMID: 32464425]
L02	IC₅₀	11.9 μM Compound: Beta-lap	Cytotoxicity against NQO1 deficient human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against NQO1 deficient human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30508483]
L02	IC₅₀	4.54 μM Compound: Beta-lap	Cytotoxicity against human L02 cells measured after 48 hrs by MTT assay Cytotoxicity against human L02 cells measured after 48 hrs by MTT assay	[PMID: 32682198]
L02	IC₅₀	9.6 μM Compound: Beta-lap	Cytotoxicity against NQO1-deficient human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against NQO1-deficient human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33984806]
LLC-PK1	CC₅₀	2.09 μM Compound: 30	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	GI₅₀	0.3 μM Compound: beta-Lapachone	Antiproliferative activity against human LoVo cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human LoVo cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 22819765]
LoVo	IC₅₀	0.3 μM Compound: Beta-Lapachone	Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay	[PMID: 26883150]
LOX IMVI	GI₅₀	0.31 μM Compound: 1 (beta-Lapachone)	Cytotoxicity against melanoma LOXIMVI cell lines Cytotoxicity against melanoma LOXIMVI cell lines	[PMID: 11448231]
MCF7	EC₅₀	9.96 μM Compound: 4	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]
MCF7	GI₅₀	12.2 μM Compound: 10	Antiproliferative activity against human MCF7 cells measured after 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells measured after 72 hrs by SRB assay	[PMID: 35687347]
MCF7	GI₅₀	4.17 μM Compound: Beta-lap	Cytotoxicity against NQO1-rich human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay Cytotoxicity against NQO1-rich human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay	[PMID: 32464425]
MCF7	IC₅₀	0.5 μM Compound: Beta-Lapachone	Antiproliferative activity against apoptosis sensitive human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against apoptosis sensitive human MCF7 cells after 72 hrs by MTT assay	[PMID: 26883150]
MCF7	IC₅₀	0.71 μM Compound: 5	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	IC₅₀	0.8 μM Compound: 13	Cytotoxicity against human MCF7 cells after 3 days by SRB assay Cytotoxicity against human MCF7 cells after 3 days by SRB assay	[PMID: 15217280]
MDA-MB-231	IC₅₀	1.39 μM Compound: 5	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]
MDA-MB-231	IC₅₀	1.39 μM Compound: 3	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by WST-8 method Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by WST-8 method	[PMID: 37343498]
MDA-MB-231	IC₅₀	4.3 μM Compound: 3	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-435	GI₅₀	21.4 μM Compound: 1 (beta-Lapachone)	Cytotoxicity against breast MDA-MB-435 cell lines Cytotoxicity against breast MDA-MB-435 cell lines	[PMID: 11448231]
MDA-MB-435	IC₅₀	0.06 μg/mL Compound: 2b, nor-beta-lapachone	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay	[PMID: 17827021]
MDA-MB-435	IC₅₀	0.25 μM Compound: 1	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay	[PMID: 19947600]
MDA-MB-435	IC₅₀	0.25 μM Compound: beta-lap	Cytotoxicity against human MDA-MB-435 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-435 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
MDA-MB-435	IC₅₀	0.25 μM Compound: Beta-lapachone	Cytotoxicity against human MDA-MB-435 cells overexpressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-435 cells overexpressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27341379]
MDA-MB-435	IC₅₀	0.25 μM Compound: b-lapachone	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay	[PMID: 21115213]
MDCK	IC₅₀	13.5 μM Compound: beta-lap	Cytotoxicity against MDCK cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against MDCK cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
MOLM-13	GI₅₀	34.5 μM Compound: 10	Antiproliferative activity against human MOLM-13 cells measured after 72 hrs by SRB assay Antiproliferative activity against human MOLM-13 cells measured after 72 hrs by SRB assay	[PMID: 35687347]
MOLT-4	IC₅₀	0.78 μM Compound: beta-lap	Cytotoxicity against human MOLT4 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human MOLT4 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
MRC5	CC₅₀	2.09 μM Compound: 30	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]
MV4-11	GI₅₀	70.1 μM Compound: 10	Antiproliferative activity against human MV4-11 cells measured after 72 hrs by SRB assay Antiproliferative activity against human MV4-11 cells measured after 72 hrs by SRB assay	[PMID: 35687347]
NCI-H23	GI₅₀	0.76 μM Compound: 1 (beta-Lapachone)	Cytotoxicity against lung NCI-H23 cell lines Cytotoxicity against lung NCI-H23 cell lines	[PMID: 11448231]
NCI-H596	IC₅₀	23 μM Compound: beta-lap	Cytotoxicity against NQO-1 deficient human NCI-H596 cells assessed as inhibition of cell viability after 2 hrs by MTT assay Cytotoxicity against NQO-1 deficient human NCI-H596 cells assessed as inhibition of cell viability after 2 hrs by MTT assay	[PMID: 24874653]
NCI-H596	IC₅₀	27 μM Compound: Beta-lap	Cytotoxicity against NQO1-deficient human NCI-H596 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against NQO1-deficient human NCI-H596 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33984806]
NCI-H596	IC₅₀	5.06 μM Compound: Beta-lap	Antiproliferative activity against human NCI-H596 cells measured after 48 hrs by MTT assay Antiproliferative activity against human NCI-H596 cells measured after 48 hrs by MTT assay	[PMID: 32682198]
OCI-Ly1	GI₅₀	>25 μM Compound: beta-Lapachone	Antiproliferative activity against human OCI-Ly1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay Antiproliferative activity against human OCI-Ly1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay	[PMID: 38349664]
OCI-Ly3	IC₅₀	4 μM Compound: 4a	Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTT assay Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTT assay	[PMID: 26496175]
OVCAR-3	IC₅₀	1.9 μM Compound: beta-lap	Cytotoxicity against human OVCAR3 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human OVCAR3 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
OVCAR-5	GI₅₀	1.82 μM Compound: 1 (beta-Lapachone)	Cytotoxicity against ovarian OVCAR-5 cell lines Cytotoxicity against ovarian OVCAR-5 cell lines	[PMID: 11448231]
OVCAR-8	IC₅₀	1.16 μM Compound: beta-lap	Cytotoxicity against human OVCAR8 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human OVCAR8 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
OVCAR-8	IC₅₀	1.16 μM Compound: Beta-lapachone	Cytotoxicity against human OVCAR8 cells overexpressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human OVCAR8 cells overexpressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27341379]
OVCAR-8	IC₅₀	1.16 μM Compound: beta-Lapachone	Cytotoxicity against human OVCAR8 cells after 72 hrs by MTT assay Cytotoxicity against human OVCAR8 cells after 72 hrs by MTT assay	10.1039/C4MD00371C
PBMC	IC₅₀	>20.6 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: 19947600]
PBMC	IC₅₀	>20.6 μM Compound: beta-Lapachone	Cytotoxicity against human PBMC cells after 72 hrs by MTT assay Cytotoxicity against human PBMC cells after 72 hrs by MTT assay	10.1039/C4MD00371C
PBMC	IC₅₀	>20.6 μM Compound: b-lapachone	Cytotoxicity against human PBMC cells after 72 hrs by Alamar Blue assay Cytotoxicity against human PBMC cells after 72 hrs by Alamar Blue assay	[PMID: 21115213]
PBMC	IC₅₀	>20.63 μM Compound: beta-lap	Cytotoxicity against human PBMC assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human PBMC assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
PBMC	IC₅₀	>20.63 μM Compound: Beta-lapachone	Cytotoxicity against NQO1-deficient human PBMC assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against NQO1-deficient human PBMC assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27341379]
PBMC	IC₅₀	2.1 μM Compound: 14, beta-Lapachone	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	1.13 μM Compound: 4	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	GI₅₀	0.01 μM Compound: beta-Lapachone	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 22819765]
PC-3	IC₅₀	<0.01 μM Compound: Beta-Lapachone	Antiproliferative activity against apoptosis sensitive human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against apoptosis sensitive human PC3 cells after 72 hrs by MTT assay	[PMID: 26883150]
PC-3	IC₅₀	1.65 μM Compound: beta-lap	Cytotoxicity against human PC3 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
PC-3	IC₅₀	1.65 μM Compound: Beta-lapachone	Cytotoxicity against human PC3 cells overexpressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3 cells overexpressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27341379]
PC-3M	IC₅₀	1.82 μM Compound: beta-lap	Cytotoxicity against human PC3M cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3M cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
Peritoneal macrophage cell	CC₅₀	0.79 μM Compound: beta-Lapachone	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	210.3 μM Compound: 4	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	210.3 μM Compound: Beta-Lapachone	Inhibition of TPA-induced EBV-EA activation in Raji cells Inhibition of TPA-induced EBV-EA activation in Raji cells	[PMID: 17950604]
RAW264.7	IC₅₀	0.47 μM Compound: beta-LAPA	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay	[PMID: 23232148]
RAW264.7	IC₅₀	4.06 μM Compound: beta-LAPA	Cytotoxicity against mouse RAW264.7 cells assessed as cell viability after 24 hrs by MTS assay Cytotoxicity against mouse RAW264.7 cells assessed as cell viability after 24 hrs by MTS assay	[PMID: 23232148]
SF-295	GI₅₀	1.54 μM Compound: 1 (beta-Lapachone)	Cytotoxicity against CNS SF-295 cell lines Cytotoxicity against CNS SF-295 cell lines	[PMID: 11448231]
SF-295	IC₅₀	0.22 μg/mL Compound: 2b, nor-beta-lapachone	Cytotoxicity against human SF295 cells after 72 hrs by MTT assay Cytotoxicity against human SF295 cells after 72 hrs by MTT assay	[PMID: 17827021]
SF-295	IC₅₀	0.91 μM Compound: 1	Cytotoxicity against human SF295 cells after 72 hrs by MTT assay Cytotoxicity against human SF295 cells after 72 hrs by MTT assay	[PMID: 19947600]
SF-295	IC₅₀	0.91 μM Compound: beta-Lapachone	Cytotoxicity against human SF295 cells after 72 hrs by MTT assay Cytotoxicity against human SF295 cells after 72 hrs by MTT assay	10.1039/C4MD00371C
SF-295	IC₅₀	0.91 μM Compound: b-lapachone	Cytotoxicity against human SF295 cells after 72 hrs by MTT assay Cytotoxicity against human SF295 cells after 72 hrs by MTT assay	[PMID: 21115213]
SF-295	IC₅₀	0.95 μM Compound: beta-lap	Cytotoxicity against human SF295 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human SF295 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26142490]
SF-295	IC₅₀	0.95 μM Compound: Beta-lapachone	Cytotoxicity against human SF295 cells overexpressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human SF295 cells overexpressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27341379]
SK-MEL-28	GI₅₀	0.6 μM Compound: beta-Lapachone	Antiproliferative activity against human SK-MEL-28 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SK-MEL-28 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 22819765]
SK-MEL-28	IC₅₀	0.6 μM Compound: Beta-Lapachone	Antiproliferative activity against apoptosis resistant human SK-MEL-28 cells after 72 hrs by MTT assay Antiproliferative activity against apoptosis resistant human SK-MEL-28 cells after 72 hrs by MTT assay	[PMID: 26883150]
SN12C	GI₅₀	1.45 μM Compound: 1 (beta-Lapachone)	Cytotoxicity against renal SN12C cell lines Cytotoxicity against renal SN12C cell lines	[PMID: 11448231]
SW1573	GI₅₀	0.76 μM Compound: 5	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]
SW1573	GI₅₀	0.84 μM Compound: 1b, ARQ 501, beta-lapachone	Growth inhibition of human SW1573 cells by SRB assay Growth inhibition of human SW1573 cells by SRB assay	[PMID: 22560628]
T47D	GI₅₀	2.3 μM Compound: 5	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]
TMD8	GI₅₀	1 μM Compound: beta-Lapachone	Antiproliferative activity against human TMD8 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay Antiproliferative activity against human TMD8 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay	[PMID: 38349664]
U-373MG ATCC	GI₅₀	0.4 μM Compound: beta-Lapachone	Antiproliferative activity against human U373 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human U373 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 22819765]
U-373MG ATCC	IC₅₀	0.4 μM Compound: Beta-Lapachone	Antiproliferative activity against apoptosis resistant human U373 cells after 72 hrs by MTT assay Antiproliferative activity against apoptosis resistant human U373 cells after 72 hrs by MTT assay	[PMID: 26883150]
U-87MG ATCC	IC₅₀	2 μM Compound: 13	Cytotoxicity against human U87MG cells after 3 days by SRB assay Cytotoxicity against human U87MG cells after 3 days by SRB assay	[PMID: 15217280]
Vero	CC₅₀	<3.1 μM Compound: 1	Cytotoxicity against african green monkey Vero cells after 72 hrs by spectrophotometric analysis Cytotoxicity against african green monkey Vero cells after 72 hrs by spectrophotometric analysis	[PMID: 22795899]
WiDr	GI₅₀	2 μM Compound: 1b, ARQ 501, beta-lapachone	Growth inhibition of human WiDr cells by SRB assay Growth inhibition of human WiDr cells by SRB assay	[PMID: 22560628]
WiDr	GI₅₀	2 μM Compound: 5	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

β-Lapachone is a topoisomerase I inhibitor. β-Lapachone (25 μM) inhibits camptothecin-induced DNA cleavage^[1].
β-Lapachone (10-40 μM) significantly reduces the colony-forming ability of CHO cells, and is cytotoxic in S phase. β-Lapachone at above 10 μM, causes a heavy DNA-strand breaks in CHO cells^[2].
β-Lapachone (10 μM) suppresses JCPyV replication in IMR-32 cells. β-Lapachone (1.0 μM) potently affects JCPyV propagation in JCI cells. β-Lapachone (0.01-0.1 μM) inhibits VP1 production in JCI cells^[4].

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

In Vivo

β-Lapachone (0.066%) ameliorates cisplatin-induced renal injury and when in combination with cisplatin, the affect is more significant in mice. β-Lapachone increases Mre11-Rad50-Nbs1 (MRN) complex expression in mice^[3].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 4707-32-8
Appearance Solid
Molecular Weight 242.27
Formula C₁₅H₁₄O₃
Color Brown to red
SMILES

O=C(C1=C2OC(C)(C)CC1)C(C3=C2C=CC=C3)=O
Synonyms

ARQ-501; NSC-26326
Structure Classification
- Quinones
- Naphthalene Quinones
Initial Source
- Plants
- other families
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

All Cell Imaging/StainingWBFlow CytometryIFCell Proliferation/Viability Assay

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Journal Impact Factor

Nat Cell Biol

Full-length GSDME mediates pyroptosis independent from cleavage. [Abstract]

2024 Sep;26(9):1545-1557. PMID: 38997456

β-Lapachone purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2024 Sep;26(9):1545-1557. [Abstract]

HeLa cells were treated with H2O2 (1 mM), vitamin C (1 mM) or β-Lapachone (5 μM) for 5 h to show pyroptotic morphology.

β-Lapachone purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2024 Sep;26(9):1545-1557. [Abstract]

HeLa cells were treated with H2O2 (1 mM), vitamin C (1 mM) or β-Lapachone (5 μM) for 1 h to show GSDME PARylation (GSDME-PAR), GSDME conformational change.

β-Lapachone purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2024 Sep;26(9):1545-1557. [Abstract]

HeLa cells were treated with H2O2 (1 mM), vitamin C (1 mM) or β-Lapachone (5 μM) for 1 h to show lipid ROS level.

β-Lapachone purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2024 Sep;26(9):1545-1557. [Abstract]

HeLa cells were treated with H2O2 (1 mM), vitamin C (1 mM) or β-Lapachone (5 μM) for 3 h to detect GSDME PM targeting.
J Nanobiotechnology

A self-amplified nanocatalytic system for achieving "1 + 1 + 1 > 3" chemodynamic therapy on triple negative breast cancer. [Abstract]

2021 Sep 4;19(1):261. PMID: 34481495
Biomaterials

A controllable self-amplifying oxidative stress strategy for boosting noninvasive sonodynamic therapy and synergistic immunotherapy. [Abstract]

2026 Jan:324:123499. PMID: 40554218
J Control Release

Bladder cancer selective chemotherapy with potent NQO1 substrate co-loaded prodrug nanoparticles. [Abstract]

2022 May 31;347:632-648. PMID: 35618186
Cell Death Dis

RNA binding protein NKAP protects glioblastoma cells from ferroptosis by promoting SLC7A11 mRNA splicing in an m6A-dependent manner. [Abstract]

2022 Jan 21;13(1):73. PMID: 35064112
Small

Enhanced Chemodynamic Therapy Mediated by a Tumor-Specific Catalyst in Synergy with Mitophagy Inhibition Improves the Efficacy for Endometrial Cancer. [Abstract]

2023 Aug;19(33):e2301497. PMID: 37086131

β-Lapachone purchased from MedChemExpress. Usage Cited in: Small. 2023 Aug;19(33):e2301497. [Abstract]

The cell viability of NQO1^high (Ishikawa, AN3CA, HEC-1B, and KLE) and NQO1^low (HeLa, ME-180, and EEC) cells were assayed separately after β-Lapachone (β-Lap) (1-10 µM; 4 h) addition for 48 h.

β-Lapachone purchased from MedChemExpress. Usage Cited in: Small. 2023 Aug;19(33):e2301497. [Abstract]

The protein expression levels of cPARP, cCaspase-3, Cyclin D1, c-Myc, and p27 Kip1 of KLE cells 48 h after β-Lapachone (β-Lap) addition (1-8 µM; 4 h) were evaluated by immunoblots. GAPDH was used as a loading control.

β-Lapachone purchased from MedChemExpress. Usage Cited in: Small. 2023 Aug;19(33):e2301497. [Abstract]

The percentages of KLE apoptotic cells were determined by flow cytometry 24 and 48 h after β-Lapachone (β-Lap) stimulation (2-8 µM; 4 h).
Adv Healthc Mater

Enhanced cGAS-STING Activation and Immune Response by LPDAM Platform-Based Lapachone-Chemical-Photothermal Synergistic Therapy for Colorectal Cancer. [Abstract]

2025 Apr;14(11):e2403309. PMID: 40103499
Acta Biomater

A Tumor-specific ROS Self-supply Enhanced Cascade-responsive Prodrug Activation Nanosystem for Amplified Chemotherapy against Multidrug-Resistant Tumors. [Abstract]

2023 Jul 1:164:522-537. PMID: 37072069
Sens Actuators B Chem

15 December 2022, 132707.
ACS Appl Mater Interfaces

Tumor-Specific Expansion of Oxidative Stress by Glutathione Depletion and Use of a Fenton Nanoagent for Enhanced Chemodynamic Therapy. [Abstract]

2019 Aug 28;11(34):30551-30565. PMID: 31397998
ACS Appl Nano Mater

2026 Feb 19;9(9):4232-4249.
Int J Mol Sci

Identification of β-Lapachone as a Potent USP22 Inhibitor That Suppresses Cancer Stemness and Enhances Chemosensitivity in Lung Adenocarcinoma. [Abstract]

2026 Jun 19;27(12):5561. PMID: 42353275
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Biomed Pharmacother

Unlocking the effective alliance of β-lapachone and hydroxytyrosol against triple-negative breast cancer cells. [Abstract]

2024 May:174:116439. PMID: 38518601

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (103.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 8.33 mg/mL (34.38 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (10.32 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.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 20% SBE-β-CD in Saline

Solubility: 2.86 mg/mL (11.81 mM); Clear solution; Need ultrasonic and warming

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocol

Kinase Assay^[1]

DNA topoisomerase I is incubated in the presence or absence of drugs (including β-Lapachone), in 20 μL of relaxation buffer (50 mM Tris (pH 7.5). 50 mM KCl, 10 mM MgCl₂, 0.5 mM dithiothreitol, 0.5 mM EDTA, 30 μg/mL bovine serum albumin) for 30 min at 37°C. Reactions are stopped by adding 1% SDS and proteinase K (50 μg/mL). After an additional 1-h incubation at 37°C, the products are separated by electrophoresis in 1% agarose gel in TAE buffer (0.04 M tris acetate, 0.001 M EDTA). The gel is stained with ethidium bromide after electrophoresis. The photographic negative is scanned with an NIH image analysis system^[1].

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

Cell Assay^[4]

Cytotoxicity is measured by an MTT assay. IMR-32 and JCI cells are plated in 96-well microtiter plates at a concentration of 5.0 × 10⁴ (topotecan) or 2.5 × 10⁴ (β-lapachone) cells/well/100 µL medium 24 hr prior to addition of various concentrations of topotecan or β-lapachone. The cells are then incubated for 72 hr at 37°C in a CO₂ incubator. Cell proliferation is assessed using a Cell Proliferation Kit I. Experiments are performed using four independent cultures^[4].

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

Animal Administration^[3]

Male Balb/c mice are provided a commercial pellet diet and water ad libitum. After 1 week of acclimation, the mice are randomly allocated to one of the following groups (5 per group): control, β-lapachone, cisplatin (18 mg/kg, ip), and β-lapachone + cisplatin (18 mg/kg, ip). The β-lapachone groups are fed a diet containing the drug (0.066) for 2 weeks prior to cisplatin injection. All mice are sacrificed under carbon dioxide anesthesia 3 days after cisplatin injection. The blood samples are subjected to serum BUN and CRE analyses. Half of the kidney is quickly removed for histopathological and immunohistochemical (IHC) studies. The other half is stored at −70°C until western blot assay^[3].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Li CJ, et al. beta-Lapachone, a novel DNA topoisomerase I inhibitor with a mode of action different from camptothecin. J Biol Chem. 1993 Oct 25;268(30):22463-8. [Content Brief]

[2]. Vanni A, et al. DNA damage and cytotoxicity induced by beta-lapachone: relation to poly(ADP-ribose) polymerase inhibition. Mutat Res. 1998 Jun 5;401(1-2):55-63. [Content Brief]

[3]. Kim TW, et al. β-Lapachone enhances Mre11-Rad50-Nbs1 complex expression in cisplatin-induced nephrotoxicity. Pharmacol Rep. 2016 Feb;68(1):27-31. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / 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
DMSO	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

Keywords

β-Lapachone

14 Cited Publications

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β-Lapachone

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All Topoisomerase Isoforms

Biological Activity

Chemical Information

Publications (14)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

β-Lapachone Related Classifications

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