GSK872 HCl（1346546-69-7 free base）

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK-872 hydrochloride 是 RIPK3 抑制剂，高亲和力结合 RIP3 激酶结构域，IC50为1.8 nM，并抑制激酶活性，IC50为1.3 nM。GSK-872 hydrochloride 降低 RIPK3 介导的坏死 (necroptosis) 和随后的 HMGB1 的细胞质易位和表达，并改善早期脑损伤中的脑水肿和神经功能缺损。

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.

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Apoptosis

RIP kinase

RIP kinase

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2703752-81-0

419.94

C19H18ClN3O2S2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 10 mg/mL (23.81 mM; 超声助溶 (<60°C); )H2O 中的溶解度 : 2.5 mg/mL (5.95 mM; 超声助溶 (<60°C)

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

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(-20℃)

With Ice Pack

≥ 2 years