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抑制剂描述:

产品名称:Spautin 1

产品别名:见爱必信官网

英文别名:Spautin 1

靶点:Autophagy

CAS:1262888-28-7

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:Spautin 1 is an inhibitor of autophagy; inhibits USP10 and USP13 activity (IC₅₀ values are 0.6 and 0.7 μM respectively) and promotes degradation of Vps34 (class III PI 3-kinase) complexes.

溶解性:DMSO : 50 mg/mL (184.33 mM; Need ultrasonic)

体外研究:

Spautin-1 enhances imatinib mesylate (IM)-induced CmL cell apoptosis by reducing the expression of the anti-apoptotic proteins Mcl-1 and Bcl-2. The pro-apoptotic activity of spautin-1 is associated with activation of GSK3β, an important downstream effector of PI3K/AKT. Spautin-1 enhances IM-induced cytotoxicity in CmL cell line K562, decreasing the IC50 from 1 to 0.5 μM. The mechanism of spautin-1 acting on acute pancreatitis is associated with impaired autophagy inhibition.

体内研究:Spautin-1 ameliorates the pathogenesis of acute pancreatitis induced by cerulein or L-arginine. Spautin-1 pretreatment significantly diminishes the elevation of serum amylase and lipase levels, which are indicative of trypsin activity. Increasing levels of serum TNFα caused by cerulein are inhibited in the presence of spautin-1. Spautin-1 treatment can ameliorate the inflammation damage induced by cerulein, such as edema, degeneration, coagulative necrosis and infiltration of inflammatory cells.

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