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KDM5A-IN-1

Name: KDM5A-IN-1
Brand: TargetMol
SKU: T15650
Price: 149 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15650Cas No. 1905481-36-8

KDM5A-IN-1 is an orally available, potent and selective inhibitor of the pan-histidine lysine demethylase 5 KDM5, inhibiting KDM5A, KDM5B, and KDM5C with IC50 values of 45 nM, 56 nM, and 55 nM, respectively.KDM5A-IN-1 inhibits PC9 H3K4Me3, and may be useful in cancer research.

KDM5A-IN-1

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Catalog No. T15650Cas No. 1905481-36-8

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$149	-	In Stock
1 mL x 10 mM (in DMSO)	$396	6-8 weeks	6-8 weeks

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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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Batch Information

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Purity:>99.99%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	KDM5A-IN-1 is an orally available, potent and selective inhibitor of the pan-histidine lysine demethylase 5 KDM5, inhibiting KDM5A, KDM5B, and KDM5C with IC50 values of 45 nM, 56 nM, and 55 nM, respectively.KDM5A-IN-1 inhibits PC9 H3K4Me3, and may be useful in cancer research.
Targets&IC50	KDM5C:55 nM, KDM5A:45 nM, KDM5B:56 nM
In vivo	KDM5A-IN-1 (compound 50, 5 mg/kg; oral administration; female CD-1 mice) exhibits moderate clearance in mice (28 mL/min/kg), good oral bioavailability (F% 34), significantly low plasma protein binding in mice (40%), and a half-life (t1/2) of 0.4 hours[1].

Chemical Properties

Molecular Weight	290.36
Formula	C₁₅H₂₂N₄O₂
Cas No.	1905481-36-8
Smiles	CC(C)c1cc([nH]n1)C(=O)N1CC[C@H](C1)NC(=O)C1CC1
Relative Density.	1.25 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store 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: 30 mg/mL (103.32 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.89 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

	1mg	5mg	10mg	50mg
1 mM	3.4440 mL	17.2200 mL	34.4400 mL	172.2000 mL
5 mM	0.6888 mL	3.4440 mL	6.8880 mL	34.4400 mL
10 mM	0.3444 mL	1.7220 mL	3.4440 mL	17.2200 mL
20 mM	0.1722 mL	0.8610 mL	1.7220 mL	8.6100 mL
50 mM	0.0689 mL	0.3444 mL	0.6888 mL	3.4440 mL
100 mM	0.0344 mL	0.1722 mL	0.3444 mL	1.7220 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