Synonyms: compound 19 [PMID: 38316017]
Compound class:
Synthetic organic
Comment: QC-182 is a PROTAC degrader of the structurally related bromodomain-containing histone acetyltransferases E1A binding protein (p300) and CREB binding protein (CBP) [1]. p300 and CBP are therapeutic targets for the development of anti-tumour drugs. QC-182 uses thalidomide as the binding moiety to engage the cereblon E3 ligase complex, and a derivetive of inobrodib (CCS1477) named QC-125 to engage the target proteins.
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Bioactivity Comments |
DC50 for p300 degradation is 93 nM in SK-HEP-1 hepatocellular carcinoma cells, and it promotes depletion of p300 and CBP proteins in mouse SK-HEP-1 xenografts [1]. See the biological activity table for inobrodib (CCS1477), which provides potency and binding affinities for p300 and CBP. |