UNC 1999

Pricing Availability   Qty
Cat.No. 4904 - UNC 1999 | C33H43N7O2 | CAS No. 1431612-23-5
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)
Datasheet
Citations
Reviews
Literature

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.

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.

Compound Libraries

UNC 1999 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 569.74. Batch specific molecular weights may vary from batch to batch due to solvent 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

References

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


If you know of a relevant reference for UNC 1999, please let us know.

View Related Products by Product Action

View all EZH2 Inhibitors

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

Citations for UNC 1999

Citations are publications that use Tocris products.

Currently there are no citations for UNC 1999. Do you know of a great paper that uses UNC 1999 from Tocris? Please let us know.

Reviews for UNC 1999

There are currently no reviews for this product. Be the first to review UNC 1999 and earn rewards!

Have you used UNC 1999?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Stem Cells

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
Cancer Metabolism

Cancer Metabolism Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.

Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Stem Cells

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.