Chemical Structure : p300 degrader 27
CAS No.:
p300 degrader 27
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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917.08
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Formula
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C50H58F2N10O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Asem MS, et al. Nat Commun. 2026 May 6. doi: 10.1038/s41467-026-72635-x.
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