GSK'963

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.
Targets
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, 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].

Protocol

Cell Research:

[1]

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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:

[1]

+ Expand
  • Animal Models: C57BL/6 mice
  • Formulation: 6% 11-β-hydroxypropyl cyclodextrin and contained 5% DMSO
  • 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)
Ethanol 46 mg/mL (199.73 mM)
Water Insoluble

* 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
Formula

C14H18N2O

CAS No. 2049868-46-2
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID