Biochem/physiol Actions

Reversible: no

Product competes with ATP.

Primary TargetBlocker of necroptosis

EC50 = 494 nM in blocking necrosis in FADD-deficient Jurkat cells treated with TNF-α

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 of 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). Also available as a 25 mM solution in DMSO (Cat. No. 505224).

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 of 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

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)