JQAD1

Name: JQAD1
Brand: Tocris Bioscience
SKU: 7682

Tocris Bioscience, part of Bio-Techne | Catalog # 7682

COA / SDS

Potent and selective EP300 Degrader (PROTAC®)

Key Product Details

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)
Molecular Weight:	932.97

View Full Technical Details for JQAD1

Technical Data
Citations

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
InChi Key	TWCIGBYYSZQAAA-GWWVHQGYSA-N
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 for JQAD1

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

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 EP300 selectively controls the enhancer landscape of MYCN-amplified neuroblastoma. Cancer Discov. 2021 PMID: 34772733