c646

Overview

C646 is a competitive, selective inhibitor of the histone acetyltransferase (HAT) domain of EP300 (p300) and CREBBP (CBP), used as a research tool to probe p300-dependent transcriptional and epigenetic programs. It has no clinical approval or development. unverified: true — not found in OncoKB canonical drug list; slug is corpus-derived.

Evidence in the corpus

• In gallbladder cancer (GBC) cells, C646 (p300 HAT inhibitor) abrogated SEMA7A-induced invasion, EMT, and tumorsphere formation; ChIP showed that recombinant SEMA7A increased p300 occupancy and H3K27ac at the SNAI1 and ZEB1 promoters, and C646 blocked this epigenetic activation, placing p300 HAT activity downstream of the SEMA7A/ITGB1/AKT1 axis PMID:24997986.

Resistance mechanisms

Cancer types (linked)

• GBC

Sources

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