GSK2983559 (compound 3)

Synonyms: RIP2 kinase inhibitor 1, RIPK2-IN-1

GSK2983559 (compound 3, RIP2 kinase inhibitor 1, RIPK2-IN-1) is a potent inhibitor of receptor interacting protein 2 (RIP2) kinase with good kinase specificity.

GSK2983559 (compound 3) Chemical Structure

GSK2983559 (compound 3) Chemical Structure

CAS: 1579965-12-0

Selleck's GSK2983559 (compound 3) has been cited by 2 publications

Purity & Quality Control

Batch: S892701 DMSO] 5 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.97%
99.97

GSK2983559 (compound 3) Related Products

Choose Selective RIP kinase Inhibitors

Biological Activity

Description GSK2983559 (compound 3, RIP2 kinase inhibitor 1, RIPK2-IN-1) is a potent inhibitor of receptor interacting protein 2 (RIP2) kinase with good kinase specificity.
Targets
RIP2 kinase [1]
In vitro
In vitro

In a screen against nonkinase targets (Eurofins, 104 receptor and ion channel binding assays and 35 enzyme and cell-based assays), GSK2983559 is highly selective, inhibiting only melatonin receptor MT3 at a concentration under 10 μM.[1].

In Vivo
In vivo

Administration of GSK2983559 at the 7.5 and 145 mg/kg b.i.d doses exhibits efficacy similar to that of prednisolone as measured by summed colon scores in a murine 2,4,6-trinitrobenzenesulfonic acid (TNBS) induced colitis model.[1].

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03358407 Terminated
Inflammatory Bowel Diseases
GlaxoSmithKline
January 11 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 538.53 Formula

C21H23N4O7PS2

 

CAS No. 1579965-12-0 SDF --
Smiles CC(C)(C)S(=O)(=O)C1=C(C=C2C(=C1)C(=NC=N2)NC3=CC4=C(C=C3)SC=N4)OCCOP(=O)(O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 5 mg/mL ( (9.28 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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