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Tocris Bioscience™ JQAD1

Numéro de catalogue. 76825
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5 mg
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Numéro de catalogue. Quantity
76825 5 mg
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Numéro de catalogue. 76825 Fournisseur Tocris Bioscience™ Code fournisseur 7682/5
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Description

Potent and selective EP300 Degrader

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.

Spécifications

Chemical Name or Material 12-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)-N-((R)-3 '-(2-((4-fluorobenzyl)(-1,1,1-trifluoropropan-2-yl)amino)-2-oxoethyl)-2 ',4 '-dioxo-2,3-dihydrospiro[indene-1,5 '-oxazolidin]-5-yl)dodecanamide
CAS 2417097-18-6
Quantity 5 mg
Target Active Degraders
Molecular Formula C48H52F4N6O9
Purity 98%