p300 degrader 27

Chemical Structure : p300 degrader 27

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货号: PC-26727Not For Human Use, Lab Use Only.

p300 degrader 27 is a potent, paralog-selective p300 protein degrader with DC50 of 22.5 nM in U2OS cells, does not affect CBP.

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生物&药学活性

p300 degrader 27 is a potent, paralog-selective p300 protein degrader with DC50 of 22.5 nM in U2OS cells, does not affect CBP.
p300 degrader 27 preferentially ubiquitinates a unique lysine on the surface of p300 that is not present on CBP, leading to selective degradation of p300.
p300 degrader 27 shows no major impact on CBP protein level or on canonical CRBN substrates, including IKZF1, IKZF3, CK1α, and GSPT1.
p300 degrader 27 decreased the level of H3K27Ac in a dose-dependent manner in U2OS cells.
p300 degrader 27 mechanistically functions through the proteasome pathway and engage both CRBN and the p300 bromodomain.
exhibited potent antiproliferative activity in MM, AML, and NHL cell lines.
p300 degrader 27 (1 and 2.5 mg/kg b.i.d. 14 days) achieved tumor growth inhibition (TGI) in NCI-H929 and TMD8 xenograft SCID mice models.

物理化学性质&存储条件

分子量	917.08
分子式	C50H58F2N10O5
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	3-(7-(difluoromethyl)-6-(1-(2-(((1s,4r)-4-(2-(4-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)naphthalen-2-yl)ethyl)cyclohexyl)amino)-2-oxoethyl)-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-N-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide

参考文献

1. Asem MS, et al. Nat Commun. 2026 May 6. doi: 10.1038/s41467-026-72635-x.

p300 degrader 27

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p300 degrader 27

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