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JQAD1

Catalog #: 7682 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7682/5
JQAD1 | CAS No. 2417097-18-6 | Active Degraders
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Description: Potent and selective EP300 Degrader

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%

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Biological Activity

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.

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

Technical Data

M.Wt:
932.97
Formula:
C48H52F4N6O9
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2417097-18-6

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.

Additional Information

Licensing Caveats:
Sold under license from Dana-Farber Cancer Institute

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