UNC 1999

Cat. No. 4904

UNC 1999 C33H43N7O2 [1431612-23-5]

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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

Biological Activity

Potent 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 Information

This 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 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

M.Wt:
569.74
Formula:
C33H43N7O2
Solubility:
Soluble to 100 mM in 1eq. HCl and to 20 mM in DMSO
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
1431612-23-5

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 / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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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