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JQAD1

Chemical Structure : JQAD1

CAS No.: 2417097-18-6

JQAD1 ((R,S)-JQAD1)

Catalog No.: PC-20886Not For Human Use, Lab Use Only.

JQAD1 is a potent, selective PROTAC degrader of p300, demonstrate a time-dependent loss of EP300, enhancer acetylation, and transcriptional output in NB cells both in vitro and in vivo.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

JQAD1 is a potent, selective PROTAC degrader of p300, demonstrate a time-dependent loss of EP300, enhancer acetylation, and transcriptional output in NB cells both in vitro and in vivo.
JQAD1 is selective for EP300 relative to CBP.
JQAD1 (1 uM) rapidly disrupts MYCN expression and causes apoptosis in Kelly NB cells.
JQAD1 causes genome-wide loss of histone H3K27ac enriched at super-enhancers.
JQAD1 (40 mg/kg i.p. daily) causes tumor growth suppression and loss of EP300 in vivo.
JQAD1 has broad CRBN-dependent antineoplastic activity across cancer cell lines.

Physicochemical Properties

M.Wt 932.97
Formula C48H52F4N6O9
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Adam D Durbin, et al. Cancer Discov. 2022 Mar 1;12(3):730-751.

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