製品番号: HY-111941

GSK8612

31 Cited Publications

カスタマーレビュー

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.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.56%
CAS 番号: 2361659-62-1
分子式: C₁₇H₁₇BrF₃N₇O₂S
分子量:520.33

保管条件:

-20°C, protect from light

* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

GSK8612 構造式

CAS 番号: 2361659-62-1

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Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

GSK8612 is a highly selective and potent Tank-binding Kinase-1 (TBK1) inhibitor, with a pIC₅₀ of 6.8 for recombinant TBK1^[1].

IC₅₀ & Target^[1]

TBK1

6.8 (pIC₅₀)

IKK アイソフォーム固有の製品をすべて表示 :

体外実験

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.

化学情報

CAS 番号 2361659-62-1
性状 Solid
分子量 520.33
分子式 C₁₇H₁₇BrF₃N₇O₂S
Color White to off-white
SMILES

NS(C1=CC=C(CNC2=C(Br)C=NC(NC3=CN(CC(F)(F)F)N=C3C)=N2)C=C1)(=O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, protect from light

* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Publications (31)

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Cancer Cell

2026 May 21:S1535-6108(26)00220-5. PMID: 42167227
Cancer Cell

Putting the STING back into BH3-mimetic drugs for TP53-mutant blood cancers. [Abstract]

2024 May 13;42(5):850-868.e9. PMID: 38670091
Nature

Targeting TBK1 to overcome resistance to cancer immunotherapy. [Abstract]

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

Histone deacetylase 3 promotes innate antiviral immunity through deacetylation of TBK1. [Abstract]

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.
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

STING-OPTN signaling confers cytoprotection through TBK1-dependent mitophagy. [Abstract]

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.
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.
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

MARCH1 negatively regulates TBK1-mTOR signaling pathway by ubiquitinating TBK1. [Abstract]

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
Yale University

2025.
bioRxiv

2025 May 17.
University of Bonn

2025.
Res Sq

2024 Aug 06.
bioRxiv

KAT2 paralogs prevent dsRNA accumulation and interferon signaling to maintain intestinal stem cells. [Abstract]

2023 Sep 5:2023.09.04.556156. PMID: 37732252
University of Glasgow

2023.

溶剤 & 溶解度

体外:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9219 mL

9.6093 mL

19.2186 mL

5 mM

0.3844 mL

1.9219 mL

3.8437 mL

10 mM

0.1922 mL

0.9609 mL

1.9219 mL

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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

Stock Solution Working Solution

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 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.

Protocol 2

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.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 2% DMSO 40% PEG300 5% Tween-80 53% Saline

Solubility: ≥ 1 mg/mL (1.92 mM); Clear solution

Protocol 5

Add each solvent one by one: 2% DMSO 98% Corn Oil

Solubility: 1 mg/mL (1.92 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (272 KB)
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)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Thomson DW, et al. Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor. ACS Med Chem Lett. 2019 Mar 11;10(5):780-785. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

GSK8612

31 Cited Publications

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GSK8612

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Mitochondria-Targeted Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

MedChemExpress（MCE）の使用を引用している文献 GSK8612

IKK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (31)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

GSK8612

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Mitochondria-Targeted Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

MedChemExpress（MCE）の使用を引用している文献 GSK8612

IKK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (31)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

GSK8612 関連分類

HY-111941 関連分類