Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

General description

A cell-permeable, potent, and selective blocker of necroptosis (EC₅₀ = 494 nM in FADD-deficient Jurkat cells treated with TNF-α), a nonapoptotic necrotic cell death pathway mediated by death-domain receptors (DRs) that offers neuroprotection in a murine model of ischemic brain injury. Exhibits no effect on DR-induced apoptosis. Also acts as a selective and ATP-competitive inhibitor of RIP1 kinase with negligible effect on RIP2 kinase activity. Nec-1 target appears to be a critical common necroptotic step upstream of execution events and downstream of DRs. Inactive control, Nec-1i, is also available (>Cat. No. 480066).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Degterev, A., et al. 2013. Nat. Chem. Biol.9, 192.Degterev, A., et al. 2012. Cell Death Differ.20, 366.Christofferson, D.E., et al. 2012. Cell Death Dis.3, e320.Takahashi, N., et al. 2012. Cell Death Dis.3, e437.Degterev, A., et al. 2008. Nat. Chem. Biol.4, 313.Degterev, A., et al. 2005. Nat. Chem. Biol.1, 112.Muller, A.J., et al. 2005. Nat. Med.11, 312.Teng, X., et al. 2005. Bioorg. Med. Chem. Lett.15, 5039.

Packaging

Packaged under inert gas

Physical form

A 25 mM (10 mg/1.54 ml) sterile-filtered solution of Necrostatin-1 (Cat. No. 480065) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 1 year at -70°C.

Warning

Toxicity: Irritant (B)