Chemical Structure : JQAD1
CAS No.: 2417097-18-6
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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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.
M.Wt | 932.97 | |
Formula | C48H52F4N6O9 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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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 |
1. Adam D Durbin, et al. Cancer Discov. 2022 Mar 1;12(3):730-751.
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