GSK2982772

Catalog No.S8484

GSK2982772 Chemical Structure

Molecular Weight(MW): 377.40

GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.

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Biological Activity

Description GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.
Targets
human RIP1 [1]
(Cell-free assay)
16 nM
In vitro

GSK2982772 has excellent activity in both RIP1 cellular systems, preventing TNF induced necrotic cell death, and an ulcerative colitis explant assay blocking spontaneous cytokine release[1].

In vivo

GSK2982772 exhibits approximately equivalent RIP1 FP potency against human and monkey RIP1 but was significantly less potent against nonprimate RIP1. GSK2982772 displays a good free fraction in blood in rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%). The inhibitor has a good pharmacokinetic profile across both rats and monkeys. GSK2982772 distributes into a range of tissues including the colon, liver, kidney, and heart at concentrations comparable to those of blood. However, it has low brain penetration in rat (4%) despite possessing good cell permeability, which is likely due to active extrusion of GSK2982772 from the brain via the efflux drug transporter. It is predicted that GSK2982772 has high bioavailability, moderate to low clearance with a moderate volume, and a terminal half-life in the order of 12 h[1].

Protocol

Animal Research:

[1]

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  • Animal Models: TNF/zVAD mouse model
  • Formulation: saline
  • Dosages: 3, 10, and 50 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (198.72 mM)
Ethanol 30 mg/mL (79.49 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 377.40
Formula

C20H19N5O3

CAS No. 1622848-92-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03649412 Recruiting Autoimmune Diseases GlaxoSmithKline|Quotient Sciences September 26 2018 Phase 1
NCT03649412 Recruiting Autoimmune Diseases GlaxoSmithKline|Quotient Sciences September 26 2018 Phase 1
NCT03590613 Completed Autoimmune Diseases GlaxoSmithKline July 19 2018 Phase 1
NCT03590613 Completed Autoimmune Diseases GlaxoSmithKline July 19 2018 Phase 1
NCT03305419 Completed Autoimmune Diseases GlaxoSmithKline October 11 2017 Phase 1
NCT03305419 Completed Autoimmune Diseases GlaxoSmithKline October 11 2017 Phase 1

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

Tel: +1-832-582-8158 Ext:3

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TNF-alpha Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID