2. NF-κB
  3. IKK
  4. TBK1/IKKε-IN-4

TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR.

For research use only. We do not sell to patients.

TBK1/IKKε-IN-4 Chemical Structure

TBK1/IKKε-IN-4 Chemical Structure

CAS No. : 1381930-17-1

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Based on 1 publication(s) in Google Scholar

TBK1/IKKε-IN-4 Related Antibodies

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IKK-α IKK-β IKK IKKε TBK1

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Description

TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR[1].

IC50 & Target[1]

IKKε

59 nM (IC50)

TBK1

13 nM (IC50)

In Vitro

TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays 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) treatment inhibits the 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). TBK1/IKKε-IN-4 effectively blocksTLR3-dependent IRF3 nuclear translocation in cells with an IC50 under 100 nM, but does not impair TNFR1-dependent p65 NFκB nuclear translocation with doses as high as 20 µM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TBK1/IKKε-IN-4 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCC44 cells
Concentration: 0 µM, 0.5 µM, 1 µM, 2 µM
Incubation Time: 30 minutes
Result: Was sufficient to blunt baseline AKT activity.
Molecular Weight

533.62

Formula

C28H35N7O4
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

COC1=CC=C(N2N=CC3=CN=C(NC4=CC(OCCCN5CCN(C)CC5)=C(OC)C(OC)=C4)N=C32)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 70 mg/mL (131.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8740 mL 9.3700 mL 18.7399 mL
5 mM 0.3748 mL 1.8740 mL 3.7480 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 4.75 mg/mL (8.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (47.5 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.5 mg/mL (6.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.42%

SDS (393 KB)

COA (249 KB) RP-HPLC (221 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8740 mL 9.3700 mL 18.7399 mL 46.8498 mL
5 mM 0.3748 mL 1.8740 mL 3.7480 mL 9.3700 mL
10 mM 0.1874 mL 0.9370 mL 1.8740 mL 4.6850 mL
15 mM 0.1249 mL 0.6247 mL 1.2493 mL 3.1233 mL
20 mM 0.0937 mL 0.4685 mL 0.9370 mL 2.3425 mL
25 mM 0.0750 mL 0.3748 mL 0.7496 mL 1.8740 mL
30 mM 0.0625 mL 0.3123 mL 0.6247 mL 1.5617 mL
40 mM 0.0468 mL 0.2342 mL 0.4685 mL 1.1712 mL
50 mM 0.0375 mL 0.1874 mL 0.3748 mL 0.9370 mL
60 mM 0.0312 mL 0.1562 mL 0.3123 mL 0.7808 mL
80 mM 0.0234 mL 0.1171 mL 0.2342 mL 0.5856 mL
100 mM 0.0187 mL 0.0937 mL 0.1874 mL 0.4685 mL
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TBK1/IKKε-IN-4 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TBK1/IKKε-IN-41381930-17-1IKKIκB kinaseI kappa B kinaseTBK1IKKε6-aminopyrazolopyrimidineLPSIFNβIP10IRF3AKTInhibitorinhibitorinhibit

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