GSK2982772

Catalog No.S8484

For research use only.

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

CAS No. 1622848-92-3

Selleck's GSK2982772 has been cited by 4 Publications

Purity & Quality Control

Choose Selective RIP kinase Inhibitors

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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells NEnOS4FHfW6ldHnvckBie3OjeR?= NGDvdmsyKGi{ NFrKSVlKdmirYnn0bY9vKG:oIHj1cYFvKFKLUEGgLFEhfG9iM{e1JJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgbY5{\WO2IHPlcIx{KHC{ZXnuZ5Vj[XSnZDDmc5IhOSCqcjDmc4xtd3enZDDifUBCXFBiYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhPSCqcoOgZpkhSUSSLVfsc{BtfW2rbnXzZ4Vv[2ViYYPzZZktKEmFNUCgQUAxNjByMTFOwG0v NV\MW|E{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVE3PTlpPkK4NVUyPjV7PD;hQi=>
U937 NXr0N|A4TnWwY4Tpc44h[XO|YYm= M{fSUFI1KGi{cx?= MVLJcohq[mm2aX;uJI9nKFKLUEGgbY4hcHWvYX6gWVk{PyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gWG5H[WyyaHGvVXZFNU:yaD3pcoR2[2WmIH7lZ5Jwe2m|IHHmeIVzKDJ2IHjyd{BjgSCFZXzsJHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IECuNFA3OyEQvF2u NEjY[nc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1NVY2QSd-MkixOVE3PTl:L3G+
L929 M3W1W2Z2dmO2aX;uJIF{e2G7 MUOyOEBpenN? NE\JR2VKdmirYnn0bY9vKG:oIGLJVFEhcW5ibX;1d4UhVDl{OTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hXE6IYXzwbIEwWV[GLV;wbE1qdmS3Y3XkJI5m[3Kxc3nzJIFnfGW{IEK0JIhzeyCkeTDD[YxtKFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFEvOyEQvF2u NGnXUXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1NVY2QSd-MkixOVE3PTl:L3G+
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 (from reference)

Animal Research:

[1]

  • Animal Models: TNF/zVAD mouse model
  • Dosages: 3, 10, and 50 mg/kg
  • Administration: oral administration

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 377.40
Formula

C20H19N5O3

CAS No. 1622848-92-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C2=CC=CC=C2OCC(C1=O)NC(=O)C3=NNC(=N3)CC4=CC=CC=C4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03590613 Completed Drug: GSK2982772|Drug: Placebo Autoimmune Diseases GlaxoSmithKline July 19 2018 Phase 1
NCT03305419 Completed Drug: GSK2982772 capsule|Drug: Placebo capsule Autoimmune Diseases GlaxoSmithKline October 11 2017 Phase 1
NCT02903966 Completed Drug: GSK2982772|Drug: Placebo Colitis Ulcerative GlaxoSmithKline November 15 2016 Phase 2
NCT02858492 Completed Drug: GSK2982772 60 mg|Drug: Placebo Arthritis Rheumatoid GlaxoSmithKline October 17 2016 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy GSK2982772 | GSK2982772 supplier | purchase GSK2982772 | GSK2982772 cost | GSK2982772 manufacturer | order GSK2982772 | GSK2982772 distributor