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Merbarone

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

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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

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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	L1210 cells:10 μM, Topo IIα:~40 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

Powder: -20°C for 3 years | 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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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