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KDM5-IN-1

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Catalog No. T15649Cas No. 1628210-26-3

KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.

KDM5-IN-1

KDM5-IN-1

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Purity: 99.50%
Catalog No. T15649Cas No. 1628210-26-3
KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$58In StockIn Stock
5 mg$196In StockIn Stock
10 mg$298In StockIn Stock
25 mg$475In StockIn Stock
50 mg$678In StockIn Stock
100 mg$912In StockIn Stock
500 mgPreferential-In Stock
1 mL x 10 mM (in DMSO)$139In 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:99.50%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.
Targets&IC50
PC9 H3K4Me3 cells:(EC50)0.34 μM, KDM5:15.1 nM
In vitro
KDM5-IN-1 is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 μM. KDM5-IN-1 potently inhibits KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively)[1].
In vivo
KDM5-IN-1(50 mg/kg; oral) shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50 in vivo[1].
Chemical Properties
Molecular Weight324.38
FormulaC17H20N6O
Cas No.1628210-26-3
SmilesCC(C)c1c([nH]c2c(cnn2c1=O)C#N)-c1cnn(c1)C(C)(C)C
Relative Density.1.28 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 30 mg/mL (92.48 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.17 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 mM3.0828 mL15.4140 mL30.8280 mL154.1402 mL
5 mM0.6166 mL3.0828 mL6.1656 mL30.8280 mL
10 mM0.3083 mL1.5414 mL3.0828 mL15.4140 mL
20 mM0.1541 mL0.7707 mL1.5414 mL7.7070 mL
50 mM0.0617 mL0.3083 mL0.6166 mL3.0828 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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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

Keywords

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