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Biological Activity for JQAD1
JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC®; DC50 ≤ 31.6 nM); comprises an EP300 inhibitor, A485 (Cat.No. 6387), joined by a linker to a cereblon E3 ligase ligand. JQAD1 brings about degradation of EP300 in neuroblastoma cell lines in a proteasome-dependent manner. JQAD1 suppresses both H3K27ac and EP300 expression levels and induces apoptosis. JQAD1 suppresses tumors growth in NSG mice xenografted with Kelly cells. CRC and MYCN genes are downregulated in tumors treated with JQAD1. JQAD1 exhibits no significant effect on coactivator CBP at concentrations inducing EP300 degradation.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Sold under license from Dana-Farber Cancer Institute
Technical Data for JQAD1
|Storage||Store at -20°C|
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 JQAD1
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for JQAD1
The following data is based on the product molecular weight 932.97. 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||1.07 mL||5.36 mL||10.72 mL|
|5 mM||0.21 mL||1.07 mL||2.14 mL|
|10 mM||0.11 mL||0.54 mL||1.07 mL|
|50 mM||0.02 mL||0.11 mL||0.21 mL|
References for JQAD1
References are publications that support the biological activity of the product.
Durbin et al (2021) EP300 selectively controls the enhancer landscape of MYCN-amplified neuroblastoma. Cancer Discov. PMID: 34772733
If you know of a relevant reference for JQAD1, please let us know.
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Citations for JQAD1
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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.
Targeted Protein Degradation Research Product Guide
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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.
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.
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia