Chemical Name: 1-Hydroxy-4-methyl-6-(phenylmethyl)-2-(1H)pyridinone
Biological ActivitySelective mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor (Ki = 120-190 nM). Displays >60-fold selectivity for mIDH1 (found in ~75% of gliomas) over wild type IDH1. Also inhibits D-2-hydroxyglutaric acid in cells expressing mIDH1 (EC50 = 2.4 μM). Does not display cytotoxicity towards non-cancerous human cells. Phenotypically lethal.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Crystallographic investigation and selective inhibition of mutant isocitrate dehydrogenase.
Zheng et al.
ACS Med.Chem.Lett., 2013;4:542
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