GSK8612
Based on 31 publication(s) in Google Scholar
GSK8612 is a highly selective and potent Tank-binding Kinase-1 (TBK1) inhibitor, with a pIC50 of 6.8 for recombinant TBK1.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.56%
- No. CAS: 2361659-62-1
- Fòrmula: C17H17BrF3N7O2S
- Peso molecular:520.33
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Almacenamiento:
-20°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK8612
More- Cancer Cell. 2026 May 21:S1535-6108(26)00220-5.
- Cancer Cell. 2024 May 13;42(5):850-868.e9. [Abstract]
- Nature. 2023 Mar;615(7950):158-167. [Abstract]
- Autophagy. 2026 Apr 25:1-18. [Abstract]
- Autophagy. 2025 Nov 27:1-14. [Abstract]
- Autophagy. 2025 Jul 27:1-23. [Abstract]
- Autophagy. 2022 Apr;18(4):891-908. [Abstract]
- Protein Cell. 2021 Apr;12(4):261-278. [Abstract]
- Nat Commun. 2025 Jan 28;16(1):1109. [Abstract]
- Mol Cell. 2023 Mar 16;83(6):927-941.e8. [Abstract]
- Adv Sci (Weinh). 2025 Dec 17:e09927. [Abstract]
- Cell Death Differ. 2025 Sep 1. [Abstract]
- Cell Death Dis. 2021 Jul 14;12(7):699. [Abstract]
- Cell Death Dis. 2019 Sep 18;10(10):692. [Abstract]
- Oncogene. 2026 Jun;45(23):2211-2224. [Abstract]
- Cell Chem Biol. 2026 Apr 16;33(4):461-473.e7. [Abstract]
- Cell Rep. 2026 Jun 9;45(6):117515. [Abstract]
- Cell Rep. 2024 Nov 27;43(12):115016. [Abstract]
- PLoS Biol. 2023 Mar 17;21(3):e3002039. [Abstract]
- Biochem Pharmacol. 2024 Jun 15:116373. [Abstract]
- Int Immunopharmacol. 2023 Feb:115:109706. [Abstract]
- BMC Cancer. 2024 Jul 26;24(1):902. [Abstract]
- J Immunol Res. 2022 Jul 26:2022:8873536. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- J Pharmacol Sci. 2023 Jun;152(2):103-111. [Abstract]
- Yale University. 2025.
- bioRxiv. 2025 May 17.
- University of Bonn. 2025.
- Res Sq. 2024 Aug 06.
- bioRxiv. 2023 Sep 5:2023.09.04.556156. [Abstract]
- University of Glasgow. 2023.
Customer Validation & Images
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Actividad biológica
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TBK1 6.8 (pIC50) |
GSK8612 inhibits toll-like receptor (TLR)3-induced IRF3 phosphorylation in Ramos cells and type I IFN secretion in primary human mononuclear cells. In THP1 cells, GSK8612 is able to inhibit secretion of IFNβ in response to dsDNA and cGAMP, the natural ligand for STING[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2361659-62-1
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Appearance Solid
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Peso molecular 520.33
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Fòrmula C17H17BrF3N7O2S
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Color White to off-white
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SMILES
NS(C1=CC=C(CNC2=C(Br)C=NC(NC3=CN(CC(F)(F)F)N=C3C)=N2)C=C1)(=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
Publications (31)
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Journal Impact Factor
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Most Recent
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Cancer Cell
2024 May 13;42(5):850-868.e9. PMID: 38670091 -
Nature
2023 Mar;615(7950):158-167. PMID: 36634707 -
Autophagy
Enhanced autophagy drives endothelial tight junction loss, BBB disruption, and behavioral deficits during inflammation. [Abstract]2026 Apr 25:1-18. PMID: 42003242 -
Autophagy
Regulation of pexophagy by a novel TBK1-MARCHF7-PXMP4-NBR1 axis in PEX1-depleted HeLa cells. [Abstract]2025 Nov 27:1-14. PMID: 41267209 -
Autophagy
Restricting intracellular Salmonella proliferation by coordinating p-TBK1 mediated mitophagy and xenophagy. [Abstract]2025 Jul 27:1-23. PMID: 40660474 -
Autophagy
USP19 (ubiquitin specific peptidase 19) promotes TBK1 (TANK-binding kinase 1) degradation via chaperone-mediated autophagy. [Abstract]2022 Apr;18(4):891-908. PMID: 34436957 -
Protein Cell
2021 Apr;12(4):261-278. PMID: 32772249
GSK8612 purchased from MedChemExpress. Usage Cited in: Protein Cell. 2021 Apr;12(4):261-278. [Abstract]
HEK293T cells are transiently co-transfected for 48 h with Flag-tagged HDAC3 and empty vectors or HA-tagged TBK1 expression plasmids, and treated with GSK8612 for 1 h before co-immunoprecipitation. When TBK1 is treated with its inhibitor GSK8612, the phosphorylation of HDAC3 is significantly decreased.
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Nat Commun
Activation of lysophagy by a TBK1-SCFFBXO3-TMEM192-TAX1BP1 axis in response to lysosomal damage. [Abstract]2025 Jan 28;16(1):1109. PMID: 39875384 -
Mol Cell
TNIP1 inhibits selective autophagy via bipartite interaction with LC3/GABARAP and TAX1BP1. [Abstract]2023 Mar 16;83(6):927-941.e8. PMID: 36898370 -
Adv Sci (Weinh)
TBK1 Induces the Formation of Optineurin Filaments That Condensate with Polyubiquitin and LC3 for Cargo Sequestration. [Abstract]2025 Dec 17:e09927. PMID: 41405403 -
Cell Death Differ
TAB2 controls a TAK1-independent cell death checkpoint at the level of TNFR1 complex II in the TNF pathway. [Abstract]2025 Sep 1. PMID: 40890346 -
Cell Death Dis
Antioxidant and food additive BHA prevents TNF cytotoxicity by acting as a direct RIPK1 inhibitor. [Abstract]2021 Jul 14;12(7):699. PMID: 34262020 -
Cell Death Dis
A20 protects cells from TNF-induced apoptosis through linear ubiquitin-dependent and -independent mechanisms. [Abstract]2019 Sep 18;10(10):692. PMID: 31534131 -
Oncogene
Targeting VPS4 elicits STING-driven anti-tumor immunity to suppress rhabdomyosarcoma growth. [Abstract]2026 Jun;45(23):2211-2224. PMID: 42032367 -
Cell Chem Biol
Selective degradation of TBK1 uncovers mechanistic insights into blocking ccRCC progression. [Abstract]2026 Apr 16;33(4):461-473.e7. PMID: 41950925 -
Cell Rep
2026 Jun 9;45(6):117515. PMID: 42268710 -
Cell Rep
Unveiling the physiological impact of ESCRT-dependent autophagosome closure by targeting the VPS37A ubiquitin E2 variant-like domain. [Abstract]2024 Nov 27;43(12):115016. PMID: 39607828
GSK8612 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Nov 27;43(12):115016. [Abstract]
Confocal images of HT-LC3-expressing MEFs treated with 10 μM GSK8612 for 48 h, pre-stained with MPL-TMR for 15 min, and stained for p62 and p-TBK1. Scale bars: 10 μm and 1 μm (magnified images).
GSK8612 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Nov 27;43(12):115016. [Abstract]
Immunoblot analysis of MEFs treated with 10 μM GSK8612 for the indicated periods of time was performed.
GSK8612 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Nov 27;43(12):115016. [Abstract]
Immunoblot analysis of 1% TX-100-soluble and -insoluble fractions prepared from mut/mut MEFs incubated in complete medium in the presence or absence of 10 μM GSK8612 for 48 h.
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PLoS Biol
CMPK2 is a host restriction factor that inhibits infection of multiple coronaviruses in a cell-intrinsic manner. [Abstract]2023 Mar 17;21(3):e3002039. PMID: 36930652
GSK8612 purchased from MedChemExpress. Usage Cited in: PLoS Biol. 2023 Mar 17;21(3):e3002039. [Abstract]
IPEC-J2 cells were treated with DMSO or different concentrations of GSK8612 (16 h) as indicated. The expression of CMPK2 was detected by western blot.
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Biochem Pharmacol
Polydatin attenuates diabetic renal inflammatory fibrosis via the inhibition of STING pathway. [Abstract]2024 Jun 15:116373. PMID: 38885772 -
Int Immunopharmacol
Lidocaine inhibits influenza a virus replication by up-regulating IFNα4 via TBK1-IRF7 and JNK-AP1 signaling pathways. [Abstract]2023 Feb:115:109706. PMID: 36638664 -
BMC Cancer
2024 Jul 26;24(1):902. PMID: 39061024 -
J Immunol Res
The Pharmacologically Active Alkaloid Cryptolepine Activates a Type 1 Interferon Response That Is Independent of MAVS and STING Pathways. [Abstract]2022 Jul 26:2022:8873536. PMID: 35928633 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
J Pharmacol Sci
Evaluation of intracellular signal molecules that regulate TLR4-stimulated inflammatory mediator expression in cultured rat chondrocytes. [Abstract]2023 Jun;152(2):103-111. PMID: 37169474 -
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bioRxiv
KAT2 paralogs prevent dsRNA accumulation and interferon signaling to maintain intestinal stem cells. [Abstract]2023 Sep 5:2023.09.04.556156. PMID: 37732252 -
Solvente y solubilidad
DMSO : ≥ 125 mg/mL (240.23 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (4.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
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.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 (protect from light). 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 | 1.9219 mL | 9.6093 mL | 19.2186 mL | 48.0464 mL |
| 5 mM | 0.3844 mL | 1.9219 mL | 3.8437 mL | 9.6093 mL | |
| 10 mM | 0.1922 mL | 0.9609 mL | 1.9219 mL | 4.8046 mL | |
| 15 mM | 0.1281 mL | 0.6406 mL | 1.2812 mL | 3.2031 mL | |
| 20 mM | 0.0961 mL | 0.4805 mL | 0.9609 mL | 2.4023 mL | |
| 25 mM | 0.0769 mL | 0.3844 mL | 0.7687 mL | 1.9219 mL | |
| 30 mM | 0.0641 mL | 0.3203 mL | 0.6406 mL | 1.6015 mL | |
| 40 mM | 0.0480 mL | 0.2402 mL | 0.4805 mL | 1.2012 mL | |
| 50 mM | 0.0384 mL | 0.1922 mL | 0.3844 mL | 0.9609 mL | |
| 60 mM | 0.0320 mL | 0.1602 mL | 0.3203 mL | 0.8008 mL | |
| 80 mM | 0.0240 mL | 0.1201 mL | 0.2402 mL | 0.6006 mL | |
| 100 mM | 0.0192 mL | 0.0961 mL | 0.1922 mL | 0.4805 mL |
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