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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

😃Good

Catalog No. T15650Cas No. 1905481-36-8

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

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Purity:>99.99%

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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 mother liquor preparation method and in vivo formula preparation method:

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。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

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

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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

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