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TCIP3
- Development stage
- Preclinical
- Lead developer
- Dana-Farber Cancer Institute
- Modality
- Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
- Administration
- Intraperitoneal
01
Overview
TCIP3 is a lead Lysine Acetyltransferase Transcriptional/Epigenetic Chemical Inducer of Proximity (KAT-TCIP) designed to treat diffuse large B-cell lymphoma (DLBCL). It functions as a bivalent small molecule or molecular glue that recruits the co-activating lysine acetyltransferases p300 and CBP to genomic loci controlled by the master transcriptional repressor BCL6. By inducing this proximity, TCIP3 rapidly reprograms the epigenome, driving the transcription of death-promoting genes that are normally silenced by BCL6, leading to cell cycle arrest and apoptosis. TCIP3 has demonstrated sub-nanomolar potency in vitro and robust anti-tumor efficacy in vivo, specifically targeting BCL6-dependent cancers while sparing healthy lymphocytes and fibroblasts.
- Other names
- KAT-TCIP3KAT-TCIP-3KAT-TCIP 3
02
Targets
BCL6 (B cell lymphoma 6 protein)CREBBP BD (Creb-binding protein bromodomain)EP300 BD (E1A Binding Protein p300 Bromodomain)
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