Home Apoptosis RIP kinase inhibitor - TNF-alpha inhibitor GSK2982772 For research use only.

GSK2982772

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.

GSK2982772 Chemical Structure

GSK2982772 Chemical Structure

CAS No. 1622848-92-3

Purity & Quality Control

Batch: S848401 DMSO]75 mg/mL]false]Ethanol]30 mg/mL]false]Water]Insoluble]false Purity: 99.06%
99.06

GSK2982772 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells Function assay 1 hr Inhibition of human RIP1 (1 to 375 residues) expressed in baculovirus infected insect cells preincubated for 1 hr followed by ATP addition measured after 5 hrs by ADP-Glo luminescence assay, IC50 = 0.001 μM. 28151659
U937 Function assay 24 hrs Inhibition of RIP1 in human U937 cells assessed as reduction in TNFalpha/QVD-Oph-induced necrosis after 24 hrs by Cell Titer-Glo luminescent cell viability assay, IC50 = 0.0063 μM. 28151659
L929 Function assay 24 hrs Inhibition of RIP1 in mouse L929 cells assessed as reduction in TNFalpha/QVD-Oph-induced necrosis after 24 hrs by Cell Titer-Glo luminescent cell viability assay, IC50 = 1.3 μM. 28151659
Click to View More Cell Line Experimental Data

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
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
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].
Animal Research Animal Models TNF/zVAD mouse model
Dosages 3, 10, and 50 mg/kg
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03590613 Completed
Autoimmune Diseases
GlaxoSmithKline
 July 19 2018 Phase 1
NCT03305419 Completed
Autoimmune Diseases
GlaxoSmithKline
 October 11 2017 Phase 1
NCT02903966 Completed
Colitis Ulcerative
GlaxoSmithKline
 November 15 2016 Phase 2
NCT02858492 Completed
Arthritis Rheumatoid
GlaxoSmithKline
 October 17 2016 Phase 2

Chemical Information & Solubility

Molecular Weight 377.40 Formula

C20H19N5O3
CAS No. 1622848-92-3 SDF Download GSK2982772 SDF
Smiles CN1C2=CC=CC=C2OCC(C1=O)NC(=O)C3=NNC(=N3)CC4=CC=CC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (198.72 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 30 mg/mL

Water : Insoluble


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In vivo
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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.

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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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