In vitro activity: Necrostatin 2 (also known as Necrostatin-2, Necrostatin-2 racemate, (±)-Necrostatin-2, 7-Cl-O-Nec-1 and Nec-1s, is a potent necroptosis inhibitor with EC50 of 50 nM. It is a racemic mixture that inhibits receptor-interacting protein kinase 1 (RIPK1) autophosphorylation. Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling necrosis. It can be induced in a FADD-deficient variant of human Jurkat T cells treated with TNF-alpha. Necrostatin 2 was also efficacious in an animal model of ischemic stroke. Necrostatin 2 demonstrated moderate pharmacokinetic characteristics and readily entered the central nervous system upon intravenous administration.
Kinase Assay: Necrostatin 2 (also known as Necrostatin-2, Necrostatin-2 racemate, (±)-Necrostatin-2, 7-Cl-O-Nec-1 and Nec-1s, is a potent necroptosis inhibitor with EC50 of 50 nM
Cell Assay: Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling necrosis. It can be induced in a FADD-deficient variant of human Jurkat T cells treated with TNF-a. 5-(1H-Indol-3-ylmethyl)-2-thiohydantoins and 5-(1H-indol-3-ylmethyl)hydantoins were found to be potent necroptosis inhibitors (called necrostatins). |