Beta-Lapachone

製品コードS7261 バッチS726102

化学情報

	Synonyms	β-Lapachone, ARQ-501	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₅H₁₄O₃
	分子量	242.27	CAS No.	4707-32-8
Solubility (25°C)*	体外	DMSO	33 mg/mL warmed with 50ºC water bath (136.21 mM)
		Ethanol	16 mg/mL (66.04 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Beta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.
in vitro	Beta-Lapachone inhibits DNA relaxation induced by DNA topoisomerase I in a dose-dependent manner. ^[1] Treatment of beta-lapachone (100 nM or greater) results in >95% inhibition of Topo I DNA unwinding activity compared to the DMSO control. beta-lapachone (1-5 μM) causes a block in G0/G1 of the cell cycle and induces apoptosis by locking Topo I onto DNA and blocking replication fork movement in HL-60 and three human prostate cancer (DU-145, PC-3, and LNCaP) cells. ^[2] Beta-Lapachone facilitates the migration of mouse 3T3 fibroblasts and human endothelial EAhy926 cells through different MAPK signaling pathways, and thus accelerates scrape-wound healing in vitro. ^[3] In addition, beta-Lapachone inhibits purified recombinant IDO1 activity through uncompetitive inhibition with IC50 of 0.44 μM, and beta-lapachone also exhibits superior retention of intracellular IDO1 inhibitory activity with an IC50 of 1.0 μM, partially dependent on biotransformation by NQO1. ^[4] Beta-lapachone induces programmed necrosis of NQO1+ cancer cells by NQO1-dependent reactive oxygen species (ROS) formation and PARP1 hyperactivation. [5]
in vivo	Beta-lapachone treatment (50 mg/kg) leads to potent inhibition of in vivo tumor growth in a xenograft mouse model of human ovarian cancer, and the combination of beta-lapachone and taxol produces a synergistic induction of apoptosis. ^[6] In normal and diabetic (db/db) mice, treatment of beta-lapachone results in a faster healing process than vehicle only. ^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HL-60, PC-3, DU145, and LNCaP cells
	濃度	0.005 to 50 μM
	反応時間	12 hours
	実験の流れ	IC50 calculations for each cell line are determined by DNA amount (IS) and anchorage-dependent colony formation (CF) assays. For the CF assay, cells are seeded at 500 viable cells/well in 6-well plates and incubated overnight, then treated with equal volumes of media containing beta-lapachone at final concentrations ranging from 0.005 to 50 μM in half-log increments (controls were treated with 0.25% DMSO, equivalent to the highest dose of beta-lapachonc used) for 4 hour or for continuous 12-hour exposures. Plates (3 wells/condition) are stained with crystal violet, and colonies of >50 normal-appearing cells are enumerated. IC50 values for various cells are calculated using drug doses with numbers of colonies surrounding 50% of control. For DNA assays, plates are harvested for IC50 determinations 8 days after treatment using a CytoFluor 2350 fluorescence measurement system. Six-well samplings are included in the calculation of DNA fluor units for each dose. A graph of beta-lapachone dose versus percentage control DNA in fluor units is used to calculate each IC50. All experiments are repeated at least twice, each in duplicate.
動物実験	動物モデル	Human ovarian cancer cells (36M2) are established in nude mice.
	投薬量	25–50 mg/kg
	投与方法	Intraperitoneal administration

参考

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CD38 Drives Progress of Osteoarthritis by Affecting Cartilage Homeostasis [ Front Pharmacol, 2021, 12:766909]	PubMed: 34790130
Kinetics of γH2AX and phospho-histone H3 following pulse treatment of TK6 cells provides insights into clastogenic activity [ Mutagenesis, 2021, geab014]	PubMed: 33964157
Nitazoxanide, an anti-parasitic drug, efficiently ameliorates learning and memory impairments in AD model mice. [ Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0220-1]	PubMed: 31000769
Predictions of genotoxic potential, mode of action, molecular targets, and potency via a tiered multiflow® assay data analysis strategy [ Environ Mol Mutagen, 2019, 60(6):513-533]	PubMed: 30702769
Peroxiredoxin V Reduces β-Lapachone-induced Apoptosis of Colon Cancer Cells. [ Anticancer Res, 2019, 39(7):3677-3686]	PubMed: 31262894
Investigating the Generalizability of the MultiFlow ® DNA Damage Assay and Several Companion Machine Learning Models With a Set of 103 Diverse Test Chemicals. [ Toxicol Sci, 2017, 162(1):146-166]	PubMed: 29106658

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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