GSK2983559 (compound 3)

Catalog No.S8927 Synonyms: RIP2 kinase inhibitor 1, RIPK2-IN-1

For research use only.

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

CAS No. 1579965-12-0

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

Purity & Quality Control

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 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

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].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 538.53
Formula

C21H23N4O7PS2

 

CAS No. 1579965-12-0
Storage 3 years -20°C powder
2 years -80°C in solvent
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

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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.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03358407 Terminated Drug: GSK2983559|Drug: Placebo Inflammatory Bowel Diseases GlaxoSmithKline January 11 2018 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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