GSK872 HCl（1346546-69-7 free base）

Research use only, not for human use.

GSK872 HCl（1346546-69-7 free base） (GSK2399872A) is an effective and specific RIP3 kinase inhibitor. It binds RIP3 kinase domain with high affinity (IC50: 1.8 nM) and inhibits kinase activity (IC50: 1.3 nM).

GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 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 injury.

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.

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 SAHResult: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.

——

Apoptosis

RIP kinase

RIP kinase

——

——

2703752-81-0

419.94

C19H18ClN3O2S2

>98% (HPLC)

In Vitro:?DMSO : 10 mg/mL (23.81 mM; Ultrasonic (<60°C); H2O : 2.5 mg/mL (5.95 mM; Ultrasonic (<60°C))

Cl.CC(C)S(=O)(=O)c1ccc2nccc(Nc3ccc4scnc4c3)c2c1

——

(-20℃)

With Ice Pack

≥ 2 years