GSK-872

SKU: orb1226486

Description

GSK-872 (GSK'872) is a potent and selective RIPK3 (receptor-interacting protein kinase-3) inhibitor; interferes with receptor-mediated endocytosis, entry of HIV, and synaptic vesicle recycling; attenuates rat nucleus pulposus (NP) cells death.(In Vitro):GSK-872 (GSK'872; 0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in human HT-29 cells in a concentration-dependent manner.(In Vivo):GSK-872 (25 mM; intracerebroventricular injection) can attenuate brain edema and improve neurological function following subarachnoid hemorrhage (SAH) and reduce the number of necrotic cells. GSK-872 can also decrease the protein levels of RIPK3 and MLKL, and cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein.

Key Properties

• CAS Number: 1346546-69-7
• MW: 383.49
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₇N₂O₂S₂
• SMILES: O=S(C1=CC=C2N=CC=C(NC3=CC=C(SC=N4)C4=C3)C2=C1)(C(C)C)=O
• Target: RIP kinase
• Solubility: DMSO: 71 mg/mL (185.1 mM); Ethanol: 38 mg/mL (99.1 mM); Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  Animal model: Eight weeks old Sprague-Dawley male rats with 300-320 g body weight (rat SAH model). Dosage: 25 mM/6 μL. Administration: Syringe pump (intracerebroventricular) at 30 min after SAH. Result: Attenuated brain edema, improved neurological function and decreased the number of necrotic cells in the ipsilateral cortex. Decreased the expression of RIPK3, MLKL and cytoplasmic HMGB1 at 72 h after SAH in the ipsilateral cortex.
• In Vitro:
  Cell Viability Assay Cell line: HT-29 cells. Concentration: 0.01, 0.03, 0.1, 0.3, 1, and 3 μM Incubation time: 24 hours. Result: Blocked TNF-induced necroptosis in a concentration-dependent manner.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK 872

Quick Database Links

Gene Symbol

RIP kinase