Home Apoptosis RIP kinase inhibitor GSK'963 For research use only.

GSK'963

GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.

GSK'963 Chemical Structure

GSK'963 Chemical Structure

CAS No. 2049868-46-2

Purity & Quality Control

Batch: S864201 DMSO]200 mg/mL]false]Ethanol]46 mg/mL]false]Water]Insoluble]false Purity: 99.48%
99.48

GSK'963 Related Products

Biological Activity

Description GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.
Targets
RIP1 kinase [1]
(Cell-free assay)
29 nM
In vitro
In vitro GSK'963 inhibits RIP1-dependent cell death with an IC50 of between 1 and 4 nM in human and murine cells[1].
Cell Research Cell lines BMDM
Concentrations 100 nM
Incubation Time 30 min
Method

For immunoblot analysis, BMDM pretreated with GSK'963 (100 nM), GSK'962 (100 nM) or Nec-1 (10 μM) for 30 min, are stimulated with 50 ng/ml TNF for 5 and 15 min. Lysates prepared in 1× Cell Lysis Buffer containing protease and phosphatase inhibitors are separated on 4-12% SDS-PAGE and blotted onto nitrocellulose membrane. Blots are probed for IκB, phospho-IκB, and tubulin as a loading control.
Experimental Result Images Methods Biomarkers Images PMID
Western blot α-p-RIPK1 / α-RIPK1 / α-p-p38 / α-p38 / α-p-MK2 / α-MK2 28506461
In Vivo
In vivo GSK'963 is a potent inhibitor of a TNF+zVAD-mediated lethal shock. At 2 mg/kg, GSK'963 would maintain blood concentrations above the concentration required for 90% inhibition of RIP1 activity for an extended period of time compared with Nec-1[1].
Animal Research Animal Models C57BL/6 mice
Dosages 0.2, 2 and 10 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 230.31 Formula

C14H18N2O
CAS No. 2049868-46-2 SDF --
Smiles CC(C)(C)C(=O)N1C(CC=N1)C2=CC=CC=C2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 200 mg/mL ( (868.39 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 46 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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