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GSK2983559 active metabolite

Name: GSK2983559 active metabolite
Brand: TargetMol
SKU: T5401
Price: 41 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5401Cas No. 1423186-80-4

GSK2983559 active metabolite (RIPK2-IN-1) is a potent, selective receptor-interacting protein-2 (RIP2) kinase inhibitor.

GSK2983559 active metabolite

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Purity: 99.57%

Catalog No. T5401Cas No. 1423186-80-4

GSK2983559 active metabolite (RIPK2-IN-1) is a potent, selective receptor-interacting protein-2 (RIP2) kinase inhibitor.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$41	In Stock	In Stock
5 mg	$97	In Stock	In Stock
10 mg	$155	In Stock	In Stock
25 mg	$288	In Stock	In Stock
50 mg	$538	-	In Stock
100 mg	$778	-	In Stock
1 mL x 10 mM (in DMSO)	$98	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.57%

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

GSK2983559 active metabolite AI Summary

GSK2983559 active metabolite exhibits significant bioactivity across several assays. It effectively inhibits multiple kinases, including STK10, VEGFR2, EPHA6, ABL2, and VEGFR3 at a concentration of 1 μM. The compound also shows inhibition of ERG, RIP2K, NOD2, and RIPK2 with IC50 values ranging from 2.0 nM to 26.0 nM, and of TLR9 and TLR2 with IC50 values greater than 10000.0 nM. Additionally, GSK2983559 active metabolite has high oral bioavailability in various animal models (Sprague-Dawley rat, Beagle dog, Gottingen minipig), displaying varied clearance rates and volumes of distribution. It demonstrates anti-inflammatory activity in patient-derived inflamed intestinal mucosa of Crohn's disease and ulcerative colitis and passive permeability in MDCK cells. In cancer-related assays, GSK2983559 active metabolite shows antiproliferative activity against human UCH1 cells (IC50 > 50000.0 nM) and UCH2 cells (IC50 of 30000.0 nM) after 72 hours, as measured by alamar blue assay. It inhibits EGFR in human A431 cells with an IC50 greater than 50000.0 nM, assessed by reduction in EGF-stimulated EGFR autophosphorylation after 90 minutes of preincubation. Additionally, the compound inhibits tracer 5 binding to human N-terminal nano luciferase-fused GAK in HEK293 cells at 5 μM with an inhibition rate of 0.0% after 2 hours by nanoBRET assay. In terms of cytotoxicity, it has an IC50 greater than 50000.0 nM against human WS1 cells, indicating low cytotoxicity. Furthermore, GSK2983559 active metabolite shows moderate binding affinity to C-terminal AVI-tagged GAK expressed in Escherichia coli and demonstrates strong target engagement by displacing fluorescent tracers from the N-terminus of human GAK and human RIPK2. Notably, the compound is not highly cytotoxic against human LNCAP and 22Rv1 cells based on MTS assay results..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

GSK2983559 active metabolite (RIPK2-IN-1) is a potent, selective receptor-interacting protein-2 (RIP2) kinase inhibitor.

Chemical Properties

Molecular Weight	458.55
Formula	C₂₁H₂₂N₄O₄S₂
Cas No.	1423186-80-4
Smiles	CC(C)(C)S(=O)(=O)c1cc2c(Nc3ccc4scnc4c3)ncnc2cc1OCCO
Relative Density.	1.423 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 26.5 mg/mL (57.79 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2 mg/mL (4.36 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1808 mL	10.9039 mL	21.8079 mL	109.0394 mL
5 mM	0.4362 mL	2.1808 mL	4.3616 mL	21.8079 mL
10 mM	0.2181 mL	1.0904 mL	2.1808 mL	10.9039 mL
20 mM	0.1090 mL	0.5452 mL	1.0904 mL	5.4520 mL
50 mM	0.0436 mL	0.2181 mL	0.4362 mL	2.1808 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc