GSK319347A
Based on 1 publication(s) in Google Scholar
GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM.
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- Pureté : 99.25%
- CAS No.: 862812-98-4
- Formule: C22H19N3O5S2
- Masse moléculaire:469.53
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK319347A
More
Activité biologique
Description
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TBK1 93 nM (IC50) |
IKK-ε 469 nM (IC50) |
IKK2 790 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.072 μM
Compound: 1
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Inhibition of TBK1 in HEK293 cells after 4.5 hrs by ISRE-luciferase reporter gene assay in presence of poly I:C
Inhibition of TBK1 in HEK293 cells after 4.5 hrs by ISRE-luciferase reporter gene assay in presence of poly I:C
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[PMID: 24462666] |
In Vitro
GSK319347A (Compound 1) inhibits TBK1 enzyme with an IC50 of 93 nM, which also translates into good cell potency (72 nM). Moreover, IKK-3 Inhibitor exhibits excellent selectivity against cell-cycle kinases CDK2 and AurB[1]. IKK-3 Inhibitor (Compound 13) is a novel IκB kinase 2 (IKK2) inhibitor with an IC50 of 790 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Chemical Information
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CAS No. 862812-98-4
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Appearance Solid
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Masse moléculaire 469.53
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Formule C22H19N3O5S2
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Color Light yellow to yellow
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SMILES
COC1=CC2=C(C=C1OC)N(C3=CC(OCC4=CC=CC=C4S(=O)(C)=O)=C(C#N)S3)C=N2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Theranostics
IKKε phosphorylates kindlin-2 to induce invadopodia formation and promote colorectal cancer metastasis. [Abstract]2020 Jan 16;10(5):2358-2373. PMID: 32104508
Solvant et solubilité
In Vitro:
DMSO : 45 mg/mL (95.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.25 mg/mL (4.79 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Johannes JW, et al. Discovery of 6-aryl-azabenzimidazoles that inhibit the TBK1/IKK-ε kinases. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1138-43. [Content Brief]
[2]. Xie HZ, et al. Pharmacophore modeling and hybrid virtual screening for the discovery of novel IκB kinase 2 (IKK2) inhibitors. J Biomol Struct Dyn. 2011 Aug;29(1):165-79. [Content Brief]
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. 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 | 2.1298 mL | 10.6489 mL | 21.2979 mL | 53.2447 mL |
| 5 mM | 0.4260 mL | 2.1298 mL | 4.2596 mL | 10.6489 mL | |
| 10 mM | 0.2130 mL | 1.0649 mL | 2.1298 mL | 5.3245 mL | |
| 15 mM | 0.1420 mL | 0.7099 mL | 1.4199 mL | 3.5496 mL | |
| 20 mM | 0.1065 mL | 0.5324 mL | 1.0649 mL | 2.6622 mL | |
| 25 mM | 0.0852 mL | 0.4260 mL | 0.8519 mL | 2.1298 mL | |
| 30 mM | 0.0710 mL | 0.3550 mL | 0.7099 mL | 1.7748 mL | |
| 40 mM | 0.0532 mL | 0.2662 mL | 0.5324 mL | 1.3311 mL | |
| 50 mM | 0.0426 mL | 0.2130 mL | 0.4260 mL | 1.0649 mL | |
| 60 mM | 0.0355 mL | 0.1775 mL | 0.3550 mL | 0.8874 mL | |
| 80 mM | 0.0266 mL | 0.1331 mL | 0.2662 mL | 0.6656 mL |
GSK319347A Related Classifications
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