Cat. No. 5244
Chemical Name: 1-Hydroxy-4-methyl-6-(phenylmethyl)
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.
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Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Zheng et al (2013) Crystallographic investigation and selective inhibition of mutant isocitrate dehydrogenase. ACS Med.Chem.Lett. 4 542. PMID: 23795241.
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Keywords: TC-E 5008, supplier, TC-E5008, selective, mutant, isocitrate, dehydrogenase, 1, (IDH1), inhibitors, inhibits, phenotypically, lethal, cancer, gliomas, D-2-hydroxyglutaric, acid, Tocris Bioscience, Other Dehydrogenase Inhibitor products