Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models

Cell Death Dis. 2012 Nov 29;3(11):e437. doi: 10.1038/cddis.2012.176.

Abstract

Necrostatin-1 (Nec-1) is widely used in disease models to examine the contribution of receptor-interacting protein kinase (RIPK) 1 in cell death and inflammation. We studied three Nec-1 analogs: Nec-1, the active inhibitor of RIPK1, Nec-1 inactive (Nec-1i), its inactive variant, and Nec-1 stable (Nec-1s), its more stable variant. We report that Nec-1 is identical to methyl-thiohydantoin-tryptophan, an inhibitor of the potent immunomodulatory enzyme indoleamine 2,3-dioxygenase (IDO). Both Nec-1 and Nec-1i inhibited human IDO, but Nec-1s did not, as predicted by molecular modeling. Therefore, Nec-1s is a more specific RIPK1 inhibitor lacking the IDO-targeting effect. Next, although Nec-1i was ∼100 × less effective than Nec-1 in inhibiting human RIPK1 kinase activity in vitro, it was only 10 times less potent than Nec-1 and Nec-1s in a mouse necroptosis assay and became even equipotent at high concentrations. Along the same line, in vivo, high doses of Nec-1, Nec-1i and Nec-1s prevented tumor necrosis factor (TNF)-induced mortality equally well, excluding the use of Nec-1i as an inactive control. Paradoxically, low doses of Nec-1 or Nec-1i, but not Nec -1s, even sensitized mice to TNF-induced mortality. Importantly, Nec-1s did not exhibit this low dose toxicity, stressing again the preferred use of Nec-1s in vivo. Our findings have important implications for the interpretation of Nec-1-based data in experimental disease models.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Disease Models, Animal
  • Drug Therapy
  • Enzyme Inhibitors / administration & dosage
  • Enzyme Inhibitors / chemistry
  • Female
  • Humans
  • Imidazoles / administration & dosage*
  • Imidazoles / chemistry*
  • Indoleamine-Pyrrole 2,3,-Dioxygenase / antagonists & inhibitors
  • Indoles / administration & dosage*
  • Indoles / chemistry*
  • Mice
  • Mice, Inbred C57BL
  • Models, Molecular
  • Molecular Structure
  • Receptor-Interacting Protein Serine-Threonine Kinases / antagonists & inhibitors
  • Species Specificity
  • Systemic Inflammatory Response Syndrome / drug therapy*

Substances

  • Enzyme Inhibitors
  • Imidazoles
  • Indoleamine-Pyrrole 2,3,-Dioxygenase
  • Indoles
  • necrostatin-1
  • Receptor-Interacting Protein Serine-Threonine Kinases