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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: ≥99% (HPLC)
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.
External Portal Information for UNC 1999
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.
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.
Technical Data for UNC 1999
| M. Wt | 569.74 |
| Formula | C33H43N7O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (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 Data 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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Product Datasheets for UNC 1999
References for UNC 1999
References are publications that support the biological activity of the product.
Konze et al (2013) An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem.Biol. 8 1324 PMID: 23614352
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
Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761
If you know of a relevant reference for UNC 1999, please let us know.
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Keywords: UNC 1999, UNC 1999 supplier, UNC1999, potent, selective, EZH2, EZH1, histone, methyltransferase, inhibitors, inhibits, UNC2400, sgc, PRC2, polycomb, repressive, complex, 2, Lysine, Methyltransferases, 4904, Tocris Bioscience
1 Citation for UNC 1999
Citations are publications that use Tocris products. Selected citations for UNC 1999 include:
Chagraoui et al (2018) SCL/TAL1 cooperates with Polycomb RYBP-PRC1 to suppress alternative lineages in blood-fated cells. Nat Commun 9 5375 PMID: 30560907
Do you know of a great paper that uses UNC 1999 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
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