TCIP3 is a bivalent molecular glue degrader that binds dually to p300/CBP and BCL6. TCIP3 redirects p300 and CBP, thereby activating programmed cell death genes that are normally repressed by the oncogenic driver gene BCL6. TCIP3 induces acetylation of BCL6 and histone tails, inhibits c-MYC transcription. TCIP3 can be used for the research of diffuse large B-cell lymphoma (DLBCL) [1].
In Vitro, TCIP3 (1-10 nM; 1-24 h) mediates rapid, potent, and ternary complex-dependent c-MYC inhibition in SUDHL5 cells; in lymphoma and leukemia cell lines, the degree of c-MYC inhibition correlates directly with BCL6 expression levels, while this inhibitory effect is significantly attenuated in cell lines with c-MYC chromosomal rearrangement[1].
References:
[1]. Nix MN, et al. A Bivalent Molecular Glue Linking Lysine Acetyltransferases to Oncogene-induced Cell Death. bioRxiv. 2025 Mar 17.
In Vitro, TCIP3 (1-10 nM; 1-24 h) mediates rapid, potent, and ternary complex-dependent c-MYC inhibition in SUDHL5 cells; in lymphoma and leukemia cell lines, the degree of c-MYC inhibition correlates directly with BCL6 expression levels, while this inhibitory effect is significantly attenuated in cell lines with c-MYC chromosomal rearrangement[1].
References:
[1]. Nix MN, et al. A Bivalent Molecular Glue Linking Lysine Acetyltransferases to Oncogene-induced Cell Death. bioRxiv. 2025 Mar 17.