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CBL0137

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Catalog No. T4126Cas No. 1197996-80-7
Alias Curaxin 137, CBLC137

CBL0137 (Curaxin 137), a metabolically stable curaxin, activates p53 (EC50: 0.37 μM) and inhibits NF-κB (EC50: 0.47 μM). It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates the efficacy of gemcitabine in preClinicalal models of pancreatic cancer.

CBL0137

CBL0137

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Purity: 99.68%
Catalog No. T4126Alias Curaxin 137, CBLC137Cas No. 1197996-80-7
CBL0137 (Curaxin 137), a metabolically stable curaxin, activates p53 (EC50: 0.37 μM) and inhibits NF-κB (EC50: 0.47 μM). It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates the efficacy of gemcitabine in preClinicalal models of pancreatic cancer.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$44In StockIn Stock
5 mg$135In StockIn Stock
10 mg$217In StockIn Stock
25 mg$436In StockIn Stock
50 mg$591-In Stock
100 mg$787-In Stock
1 mL x 10 mM (in DMSO)$116In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.68%
Appearance:Solid
Color:White to Yellow
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Product Introduction

CBL0137 AI Summary
CBL0137 is a molecule that exhibits various bioactivities related to DNA binding and inhibition of DNA methylation mediated by the murine DNMT3A catalytic domain. It shows significant binding affinity to different 30-mer duplex DNA sequences with varying dissociation constants (Kd) and demonstrates the ability to inhibit the DNA methylation process catalyzed by DNMT3A, as indicated by its IC50 values. Additionally, it interacts with the murine DNMT3A catalytic domain, forming enzyme-DNA complexes. Overall, CBL0137 displays potent bioactivities in the context of DNA binding and inhibition of DNA methylation processes..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
CBL0137 (Curaxin 137), a metabolically stable curaxin, activates p53 (EC50: 0.37 μM) and inhibits NF-κB (EC50: 0.47 μM). It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates the efficacy of gemcitabine in preClinicalal models of pancreatic cancer.
Targets&IC50
p53:0.37 μM (EC50), NF-κB:0.47 μM (EC50)
SynonymsCuraxin 137, CBLC137
Chemical Properties
Molecular Weight336.43
FormulaC21H24N2O2
Cas No.1197996-80-7
SmilesC(CNC(C)C)N1C=2C(C=3C1=CC=C(C(C)=O)C3)=CC(C(C)=O)=CC2
Relative Density.no data available
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 25 mg/mL (74.31 mM), Sonication is recommended.
H2O: Insoluble
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.94 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.9724 mL14.8619 mL29.7239 mL148.6193 mL
5 mM0.5945 mL2.9724 mL5.9448 mL29.7239 mL
10 mM0.2972 mL1.4862 mL2.9724 mL14.8619 mL
20 mM0.1486 mL0.7431 mL1.4862 mL7.4310 mL
50 mM0.0594 mL0.2972 mL0.5945 mL2.9724 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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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

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