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C-646
- Development stage
- Preclinical
- Lead developer
- Johns Hopkins University
- Modality
- Small Molecules
- Administration
- Oral, Intraperitoneal, Intrathecal
01
Overview
C-646 is a selective, small-molecule inhibitor of the lysine acetyltransferases p300 and CBP (CREB-binding protein). It functions as a competitive inhibitor of acetyl-CoA binding to the p300 catalytic domain, thereby reducing the acetylation of histones and other non-histone proteins. In preclinical research, C-646 has been investigated for its potential to overcome resistance to Bruton's tyrosine kinase (BTK) inhibitors in mantle cell lymphoma (MCL) by suppressing NFκB activity and AKT phosphorylation. While widely utilized as a chemical probe to study epigenetic regulation and gene expression in various cancers, C-646 is primarily a research-use-only tool and has not advanced into clinical development.
- Other names
- C646C-646C 646
02
Targets
HDAC (HDAC family)CREBBP (CREB-binding protein)EP300 (Histone acetyltransferase p300)
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