UNC 1999
Chemical Name: N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide
Purity: ≥99%
Biological Activity
UNC 1999 is a potent and SAM-competitive EZH2/EZH1 lysine methyltransferase inhibitor (IC50 values are 10 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.Negative Control also available.
External Portal Information
Chemicalprobes.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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.
Scheer et al.
Nat.Commun., 2019;10:19 -
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.
Konze et al.
ACS Chem.Biol., 2013;8:1324 -
Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia.
Xu et al.
Blood, 2015;125:346
Product Datasheets
Citation for UNC 1999
The citations listed below are publications that use Tocris products. Selected citations for UNC 1999 include:
1 Citation: Showing 1 - 1
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SCL/TAL1 cooperates with Polycomb RYBP-PRC1 to suppress alternative lineages in blood-fated cells.
Authors: Chagraoui Et al.
Nat Commun 2018;9:5375
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