Home Apoptosis RIP kinase inhibitor GSK'963

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GSK'963 RIP kinase inhibitor

Cat.No.S8642

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 RIP kinase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 230.31

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 230.31 Formula

C14H18N2O

 Storage (From the date of receipt)
CAS No. 2049868-46-2 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(C)(C)C(=O)N1C(CC=N1)C2=CC=CC=C2

Solubility

In vitro
Batch:

DMSO : 200 mg/mL (868.39 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

Mechanism of Action

Targets/IC50/Ki
RIP1 kinase [1]
(Cell-free assay)
29 nM
In vitro
GSK'963 inhibits RIP1-dependent cell death with an IC50 of between 1 and 4 nM in human and murine cells[1].
In vivo
GSK'963 is a potent inhibitor of a TNF+zVAD-mediated lethal shock. At 2 mg/kg, this compound 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].
References

Applications

Methods Biomarkers Images PMID
Western blot α-p-RIPK1 / α-RIPK1 / α-p-p38 / α-p38 / α-p-MK2 / α-MK2 S8642-WB1/ 28506461

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