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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

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 recommeded.

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 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

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