JQAD1

Tocris Bioscience | Catalog # 7682

Potent and selective EP300 Degrader (PROTAC®)
Tocris Bioscience

Key Product Details

Description

Potent and selective EP300 Degrader (PROTAC®)
View all Active Degraders »

Product Description

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

Product Specifications for JQAD1

Molecular Weight

932.97

Formula

C48H52F4N6O9

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

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

Calculators

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Background References

References are publications that support the biological activity of the product.

Product Documents for JQAD1

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for JQAD1

For research use only

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