UNC 1999
Tocris Bioscience, part of Bio-Techne | Catalog # 4904
Potent and selective EZH2/EZH1 inhibitor
Product Description
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.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.Product Specifications
Molecular Weight
569.74
Formula
C33H43N7O2
Storage
Store at +4°C
Purity
≥98% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.39 | 20 | |
| 1M HCl | 56.97 | 100 |
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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for UNC 1999
For research use only
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