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TBK1/IKKε-IN-4

Name: TBK1/IKKε-IN-4
Brand: TargetMol
SKU: T38263
Rating: 4.5 (1 reviews)

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Catalog No. T38263Cas No. 1381930-17-1

Alias TBK1/IKKε-IN-4

TBK1/IKKε-IN-4, a 6-aminopyrazolopyrimidine derivative, serves as a potent, selective inhibitor for TBK1 and IKKε, demonstrating IC50 values of 13 nM and 59 nM, respectively. This compound exhibits significantly reduced activity, by 100- to 1000-fold, against other protein kinases, such as PDK1, PI3K family members, and mTOR[1].

TBK1/IKKε-IN-4

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Catalog No. T38263Alias TBK1/IKKε-IN-4Cas No. 1381930-17-1

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,520	6-8 weeks	6-8 weeks
50 mg	$1,980	6-8 weeks	6-8 weeks
100 mg	$2,500	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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Product Introduction

Bioactivity

Description	TBK1/IKKε-IN-4, a 6-aminopyrazolopyrimidine derivative, serves as a potent, selective inhibitor for TBK1 and IKKε, demonstrating IC50 values of 13 nM and 59 nM, respectively. This compound exhibits significantly reduced activity, by 100- to 1000-fold, against other protein kinases, such as PDK1, PI3K family members, and mTOR[1].
Targets&IC50	TBK1:13 nM (IC50), IKKε:59 nM (IC50)
In vitro	TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 and HCC44 cells) demonstrates selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells)[1]. TBK1/IKKε-IN-4 (Compound II; 0-2 μM; 30 minutes; HCC44 cells) inhibits AKT activity[1]. TBK1/IKKε-IN-4 (Compound II) inhibits LPS-induced expression of IFNβ (IC50 = 62 nM) and the IFNβ target genes IP10 (IC50 = 78 nM) and Mx1 (IC50 = 20 nM). It effectively blocks TLR3-dependent IRF3 nuclear translocation (IC50 < 100 nM) without impairing TNFR1-dependent p65 NFκB nuclear translocation at doses up to 20 μM[1].
Synonyms	TBK1/IKKε-IN-4

Chemical Properties

Molecular Weight	533.62
Formula	C₂₈H₃₅N₇O₄
Cas No.	1381930-17-1
Smiles	COc1ccc(cc1)-n1ncc2cnc(Nc3cc(OC)c(OC)c(OCCCN4CCN(C)CC4)c3)nc12

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: 70 mg/mL (131.18 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.18 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	1.8740 mL	9.3700 mL	18.7399 mL	93.6996 mL
5 mM	0.3748 mL	1.8740 mL	3.7480 mL	18.7399 mL
10 mM	0.1874 mL	0.9370 mL	1.8740 mL	9.3700 mL
20 mM	0.0937 mL	0.4685 mL	0.9370 mL	4.6850 mL
50 mM	0.0375 mL	0.1874 mL	0.3748 mL	1.8740 mL
100 mM	0.0187 mL	0.0937 mL	0.1874 mL	0.9370 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