Cat. No. 4904
Chemical Name: N-[(1,2-Dihydro-6-methyl-2-oxo-4-pr
Biological ActivityPotent and SAM-competitive EZH2/EZH1 lysine methyltransferase inhibitor (IC50 values are 2 and 45 nM respectively). Selective for EZH2/EZH1 over a panel of other methyltransferases and non-epigenetic targets. Reduces H3K27me3 levels in vitro. Prolongs survival of MLL-AF9 bearing mice. Orally bioavailable.
Licensing InformationThis probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the UNC 1999 probe summary on the SGC website.
External Portal InformationChemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of UNC 1999 is reviewed on the chemical probes website.
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.
Certificate of Analysis / Safety Data Sheet
Xu et al (2015) Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood 125 346. PMID: 25395428.
Konze et al (2013) An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem.Biol. 8 1324. PMID: 23614352.
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Keywords: UNC 1999, supplier, UNC1999, potent, selective, EZH2, EZH1, histone, methyltransferase, inhibitors, inhibits, UNC2400, sgc, Tocris Bioscience, Lysine Methyltransferase Inhibitor products
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