GSK8612

Name: GSK8612
Brand: MedChemExpress
SKU: HY-111941
Rating: 5.0 (16 reviews)

Cat. No.: HY-111941 Purity: 99.62%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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

GSK8612 Chemical Structure

CAS No. : 2361659-62-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 120	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 120	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 105	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 825	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 16 publication(s) in Google Scholar

15 Publications Citing Use of MCE GSK8612

: 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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IKK-α IKK-β IKK IKKε TBK1

Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

In Vitro

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.

Molecular Weight

520.33

Formula

C₁₇H₁₇BrF₃N₇O₂S

CAS No.

2361659-62-1

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

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

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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 (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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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, 2 years; -20°C, 1 year (protect from 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: 99.62%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (247 KB) HNMR (268 KB) RP-HPLC (244 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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]

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

GSK8612 Related Classifications

NF-κB
IKK

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:

GSK86122361659-62-1GSK 8612GSK-8612IKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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GSK8612

Customer Review

GSK8612 Related Antibodies

15 Publications Citing Use of MCE GSK8612

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All IKK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

GSK8612 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GSK8612 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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