ネクロスタチン-1

外観

うすい黄赤色～黄色～緑色粉末～結晶

使用

Necrostatin-1 is a specific RIP1 inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM.

生物活性

ATP-competitive death domain receptor-associated adaptor kinase (RIP1) allosteric inhibitor (EC 50 = 182 nM). Blocks non-apoptotic cell death via inhibition of a specific cellular pathway, necroptosis, which leads to necrosis (EC 50 = 494 nM). Reduces ischemic brain injury in a mouse model of stroke.

Biochem/physiol Actions

Necrostatin-1(Nec-1) might exhibit therapeutic benefit against patients with traumatic brain injury (TBI). In addition, it might also be used to treat other acute central nervous system (CNS) disorders that feature necroptosis as a mode of cell death. It is extensively used to study the effect of receptor-interacting protein kinase 1 (RIPK1) on cell death and inflammation in experimental disease models. Nec‐1 protects hippocampal (HT‐22) cells from glutamate‐induced oxytosis via increasing cellular glutathione (GSH) levels, decreasing reactive oxygen species production, inhibiting the nuclear translocation of apoptosis‐inducing factor and B-cell lymphoma 2 (Bcl‐2) /adenovirus E1B 19kDa‐interacting protein 3‐related pathways.