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Description: Potent and selective EP300 Degrader (PROTAC®)
Chemical Name: 12-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)-N-((R)-3'-(2-((4-fluorobenzyl)((S)-1,1,1-trifluoropropan-2-yl)amino)-2-oxoethyl)-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-oxazolidin]-5-yl)dodecanamide
Purity: ≥98% (HPLC)
Literature (2)

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 tumor 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.

p300 antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF3789.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Technical Data for JQAD1

M. Wt 932.97
Formula C48H52F4N6O9
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2417097-18-6
PubChem ID 162615894
Smiles C[C@@H](C(F)(F)F)N(C(CN1C(O[C@]2(C1=O)CCC3=CC(NC(CCCCCCCCCCCNC4=CC=C5C(N(C(C5=C4)=O)C6CCC(NC6=O)=O)=O)=O)=CC=C23)=O)=O)CC7=CC=C(C=C7)F

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
DMSO 93.3 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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.

Keywords: JQAD1, JQAD1 supplier, EP300, PROTAC, PROTACs, active, degraders, degrades, histone, acetyltransferase, proteolysis-targeting, chimera, prostate, cancer, potent, selective, Histone, Acetyltransferases, CBP, and, p300, Degraders, 7682, Tocris Bioscience

Citations for JQAD1

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Literature in this Area

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Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Targeted Protein Degradation Poster

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