UNC 1999

Name: UNC 1999
Brand: Tocris Bioscience
SKU: 4904

Tocris Bioscience, part of Bio-Techne | Catalog # 4904

Citations (21)

COA / SDS

Potent and selective EZH2/EZH1 inhibitor

Key Product Details

Description:	Potent and selective EZH2/EZH1 inhibitor
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:	≥98% (HPLC)
Molecular Weight:	569.74

View Full Technical Details for UNC 1999

Technical Data
Citations

Biological Activity for UNC 1999

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.

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.

Compound Libraries for UNC 1999

UNC 1999 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

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 for UNC 1999

M. Wt	569.74
Formula	C₃₃H₄₃N₇O₂
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	1431612-23-5
PubChem ID	72551585
InChi Key	DPJNKUOXBZSZAI-UHFFFAOYSA-N
Smiles	CC(C)N1CCN(C2=NC=C(C3=CC(N(C(C)C)N=C4)=C4C(C(NCC5=C(CCC)C=C(C)NC5=O)=O)=C3)C=C2)CC1

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.

Solubility for UNC 1999

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	1M HCl	56.97	100
	DMSO	11.39	20

Preparing Stock Solutions for UNC 1999

The following data is based on the product molecular weight 569.74.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.76 mL	8.78 mL	17.55 mL
5 mM	0.35 mL	1.76 mL	3.51 mL
10 mM	0.18 mL	0.88 mL	1.76 mL
50 mM	0.04 mL	0.18 mL	0.35 mL

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References for UNC 1999

References are publications that support the biological activity of the product.

Xu Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood 2015 PMID: 25395428
Scheer A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 2019 PMID: 30604761
Konze An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem.Biol. 2013 PMID: 23614352