2. NF-κB
  3. IKK
  4. TBK1/IKKε-IN-5

TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity.

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

TBK1/IKKε-IN-5 Chemical Structure

TBK1/IKKε-IN-5 Chemical Structure

CAS No. : 1893397-65-3

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5 mg USD 410 In-stock
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TBK1/IKKε-IN-5 Related Antibodies

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IKK-α IKK-β IKK IKKε TBK1

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Description

TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity[1].

IC50 & Target

IC50: 1 nM (TBK1), 5.6 nM (IKKε)[1].
In Vitro

TBK1/IKKε-IN-5 (0.001-10 µM; 24 or 96 h) promotess secretion of IL-2 and IFN-γ in purified CD4+ and CD8+ T cells and IL-2 in Jurkat human T-cell leukemia cells[1].
TBK1/IKKε-IN-5 effectively blocks immune suppressive cytokine elaboration by CT26 cell line spheroids, without cytotoxic effects[1].

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

TBK1/IKKε-IN-5 Related Antibodies

Cell Viability Assay[1]

Cell Line: CD4+ and CD8+ T cells, Jurkat T cell leukemia cells
Concentration: 0.001-10 µM
Incubation Time: 24 h (for IL-2); 96 h(for IFN-γ)
Result: Enhanced secretion of IL-2 and IFN-γ.
In Vivo

TBK1/IKKε-IN-5 (40 mg/kg; p.o.; single daily for 26 days) shows good antitumor activity and prolongs survival, as well as induces immunologic memory of CT26 cells in mice when combines with anti-PD-L1[1].

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

Animal Model: Female Balb/c mice (11 to 12-week-old; bearing CT26 tumors)[1].
Dosage: 40 mg/kg
Administration: Oral gavage; single daily for 26 days (combine with anti-PD-L1).
Result: Exhibited greater tumor control and longer survival when combined with anti-PD-L1 than used alone of both agents
Induced immunologic memory of CT26 cells in mice when combined with anti-PD-L1.
Molecular Weight

513.59

Formula

C28H31N7O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

N#CC1=CC(C2=NC(NC3=CC=C(N4CCN(C5COC5)CC4)C=C3)=NC=N2)=CC=C1OC6CCOCC6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 7.81 mg/mL (15.21 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 1.9471 mL 9.7354 mL 19.4708 mL
5 mM 0.3894 mL 1.9471 mL 3.8942 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.58%

COA (246 KB) LCMS (266 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9471 mL 9.7354 mL 19.4708 mL 48.6770 mL
5 mM 0.3894 mL 1.9471 mL 3.8942 mL 9.7354 mL
10 mM 0.1947 mL 0.9735 mL 1.9471 mL 4.8677 mL
15 mM 0.1298 mL 0.6490 mL 1.2981 mL 3.2451 mL
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TBK1/IKKε-IN-5 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-51893397-65-3IKKIκB kinaseI kappa B kinaseCT26CD4+CD8+ T cellsIL-2IFN-γCT26 tumorPD-L1combined immunizationInhibitorinhibitorinhibit

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