GSK963

SKU: orb1302135

Description

GSK963

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 2049868-46-2
• MW: 230.31
• Purity: 98.00%
• Formula: C₁₄H₁₈N₂O
• SMILES: CC(C)(C)C(=O)N1N=CC[C@H]1c1ccccc1
• Target: RIP kinase
• Solubility: DMSO:40 mg/mL (173.68 mM);10% DMSO+90% Corn Oil:2 mg/mL (8.68 mM)

Bioactivity

• Target IC50:
  RIP1:29 nM
• In Vivo:
  GSK 963 efficiently blocked necroptosis in both murine and human cells with IC50 values of 1 nM and 4 nM, respectively, whereas the inactive analog GSK 962 was at least 1000-fold less potent in these assays.
• In Vitro:
  The increased potency of GSK 963 relative to Nec-1 in vitro also translated into increased efficacy in the TNF+zVAD-induced model of sterile shock. At a dose of 2 mg/kg, GSK 963 was able to completely inhibit temperature loss in response to TNF+zVAD, the phenotype of the recently described RIP1 kinase-dead knock-in mice. The level of inhibition of temperature loss in this acute model at different doses of GSK 963 was in line with the predictions of efficacy based on modeling of the pharamacokinetic profile and in vitro potency of GSK 963.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK 963, GSK963, GSK-963, GSK963 (Racemate), Racemate, RIPkinase, RIP kinase, RIP1

Compound Identifiers

PubChem CID

122703613