GSK-872

SKU: orb1690387

Description

GSK-872 is a potent and selective RIP3 kinase inhibitor, exhibiting high-affinity binding and inhibitory activity in the low nanomolar range. This compound is a valuable research tool for investigating necroptosis in both cellular and animal models, aiding the study of inflammatory and neurodegenerative diseases.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1346546-69-7
• MW: 383.49
• Purity: >99.99% (May vary between batches)
• Formula: C₁₉H₁₇N₃O₂S₂
• SMILES: CC(C)S(=O)(=O)c1ccc2nccc(Nc3ccc4scnc4c3)c2c1
• Target: RIP kinase
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:141 mg/mL (367.68 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.43 mM);Ethanol:38 mg/mL (99.09 mM)

Bioactivity

• Target IC50:
  RIP3K:1.8 nM
• In Vivo:
  In compared with no treatment after ischemic injury in vivo, GSK872 can significantly reduce HIF-1α expression .
• In Vitro:
  GSK872 (1 μM) has no inhibition for most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase. In HT-29 cells, GSK872 concentration-dependently blocks TNF-induced necroptosis. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK872 inhibits DAI- or TLR3-induced (RIP1-independent) death. It induces caspase activation and then induces apoptotic cell death.

Storage & Handling

• Storage: store at low temperature | 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

Receptor-interacting protein kinases, RIP kinase, RIPK, RIP3K, RIPkinase, translocation, cytoplasmic, deficits, brain, inhibit, neurological, GSK872, GSK'872, GSK-872, GSK 872, GSK2399872A, edema, Inhibitor, HMGB1

Compound Identifiers

PubChem CID

54674134