For research use only.

Catalog No.S8642

GSK'963 Chemical Structure

Molecular Weight(MW): 230.31

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.

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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.
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].

Methods Test Index PMID
Western blot
α-p-RIPK1 / α-RIPK1 / α-p-p38 / α-p38 / α-p-MK2 / α-MK2 ; 

PubMed: 28506461     

Western blot analysis of cell lysates of the indicated cells using the described antibodies. Cells were left untreated or pre-treated for 30 min with the indicated inhibitors, followed by TNF treatment (10 ng/mL, 10 min) (SM CompA, 500 nM; RIPK1i GSK’963, 100 nM; TAK1i (5Z)-7-O, 1 μM; IKKi TPCA-1, 5 μM; p38i, 1 μM; MK2i PF3644022, 1 μM).

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].


Cell Research:


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  • 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.

    (Only for Reference)
Animal Research:


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  • Animal Models: C57BL/6 mice
  • Dosages: 0.2, 2 and 10 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 46 mg/mL (199.73 mM)
Water Insoluble
Ethanol '46 mg/mL

* 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 230.31


CAS No. 2049868-46-2
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)(C)C(=O)N1N=CCC1C2=CC=CC=C2

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID