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Synonyms: methyl-thiohydantoin-tryptophan | MTH-DL-tryptophan | MTH-trp | nec-1 | Necrostatin 1
Compound class: Synthetic organic
Comment: Necrostatin-1 is an inhibitor of necroptosis . It inhibits RIPK1  and IDO  enzyme activities .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Degterev A, Hitomi J, Germscheid M, Ch'en IL, Korkina O, Teng X, Abbott D, Cuny GD, Yuan C, Wagner G et al.. (2008)
Identification of RIP1 kinase as a specific cellular target of necrostatins.
Nat. Chem. Biol., 4 (5): 313-21. [PMID:18408713]
2. Degterev A, Huang Z, Boyce M, Li Y, Jagtap P, Mizushima N, Cuny GD, Mitchison TJ, Moskowitz MA, Yuan J. (2005)
Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury.
Nat. Chem. Biol., 1 (2): 112-9. [PMID:16408008]
3. Muller AJ, DuHadaway JB, Donover PS, Sutanto-Ward E, Prendergast GC. (2005)
Inhibition of indoleamine 2,3-dioxygenase, an immunoregulatory target of the cancer suppression gene Bin1, potentiates cancer chemotherapy.
Nat. Med., 11 (3): 312-9. [PMID:15711557]
4. Takahashi N, Duprez L, Grootjans S, Cauwels A, Nerinckx W, DuHadaway JB, Goossens V, Roelandt R, Van Hauwermeiren F, Libert C et al.. (2012)
Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models.
Cell Death Dis, 3: e437. [PMID:23190609]
5. Vandenabeele P, Grootjans S, Callewaert N, Takahashi N. (2013)
Necrostatin-1 blocks both RIPK1 and IDO: consequences for the study of cell death in experimental disease models.
Cell Death Differ., 20 (2): 185-7. [PMID:23197293]