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Merbarone

Name: Merbarone
Brand: TargetMol
SKU: T28017
Rating: 4.5 (1 reviews)

🥰Excellent

Catalog No. T28017Cas No. 97534-21-9

Alias RLBN-1001, RLBN1001, NSC-336628, NSC336628

Merbarone is a Type II DNA topoisomerase inhibitor that suppresses the catalytic activity of human topoisomerase IIα by blocking DNA cleavage, subsequently inducing activation of caspase-activated DNase and excision of chromosomal DNA loops from the nuclear matrix, Merbarone triggers apoptosis in CEM cells through activation of ICE/CED-3-like proteases, making it a mechanistically informative compound for studying DNA damage responses and apoptosis pathways.

Merbarone

🥰Excellent

Catalog No. T28017Alias RLBN-1001, RLBN1001, NSC-336628, NSC336628Cas No. 97534-21-9

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Product Introduction

Bioactivity

Description	Merbarone is a Type II DNA topoisomerase inhibitor that suppresses the catalytic activity of human topoisomerase IIα by blocking DNA cleavage, subsequently inducing activation of caspase-activated DNase and excision of chromosomal DNA loops from the nuclear matrix, Merbarone triggers apoptosis in CEM cells through activation of ICE/CED-3-like proteases, making it a mechanistically informative compound for studying DNA damage responses and apoptosis pathways.
Targets&IC50	Topo IIα:~40 μM, L1210 cells:10 μM
In vitro	In biochemical assays, Merbarone (10-200 μM) acted as a catalytic inhibitor of human Topoisomerase IIα, inhibiting DNA relaxation (IC50 ~ 40 μM) and blocking DNA cleavage (IC50 ~ 50 μM) without stabilizing the DNA-enzyme intermediate or impairing ATP hydrolysis. In cellular assays, it inhibited L1210 leukemia cell proliferation in a concentration-dependent manner with an IC50 of 10 μM [1].
In vivo	In murine leukemia models, Merbarone shows antitumor activity. Intraperitoneal (i.p.) administration of Merbarone (50 mg/kg, daily) for 5 days in mice bearing P388 leukemia resulted in a maximum Increase in Lifespan (ILS) of 101%. Furthermore, oral administration (124 mg/kg, daily) for 9 days also demonstrated tumor growth inhibition in these models [2].
Synonyms	RLBN-1001, RLBN1001, NSC-336628, NSC336628

Chemical Properties

Molecular Weight	263.27
Formula	C₁₁H₉N₃O₃S
Cas No.	97534-21-9
Smiles	O=C(NC=1C=CC=CC1)C2C(=O)NC(=S)NC2=O
Relative Density.	1.31g/cm3

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 10 mg/mL (37.98 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.7984 mL	18.9919 mL	37.9838 mL	189.9191 mL
5 mM	0.7597 mL	3.7984 mL	7.5968 mL	37.9838 mL
10 mM	0.3798 mL	1.8992 mL	3.7984 mL	18.9919 mL
20 mM	0.1899 mL	0.9496 mL	1.8992 mL	9.4960 mL

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For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline /PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Stock solution preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline /PBS/ddH₂O TargetMol | reagent

mix well and clarify

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All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc