GSK-872 hydrochloride (C09-1135-646)

GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC 50 of 1.8 nM, and inhibits kinase activity with an IC 50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injuryIn VitroGSK-872 hydrochloride (0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in human HT-29 cells in a concentration-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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.In VivoGSK-872 hydrochloride (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 hydrochloride can also decrease the protein levels of RIPK3 and MLKL, and cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.Form:SolidIC50& Target:RIPK3. Specifications and Purity: 99%. Molecular Formula: C19H18ClN3O2S2. Molecular Weight: 419.95.