JQAD1 | EP300 degrader | Probechem Biochemicals

Chemical Structure : JQAD1

CAS No.: 2417097-18-6

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JQAD1 ((R,S)-JQAD1)

货号: 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.

规格	价格	库存
5 mg	￥2580	In stock
10 mg	￥3880	In stock
25 mg	￥5880	In stock
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	932.97
分子式	C48H52F4N6O9
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

JQAD1 ((R,S)-JQAD1)

生物&药学活性

物理化学性质&存储条件

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JQAD1 ((R,S)-JQAD1)

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