BCL6 Inhibitor

BI-3812, a chemical probe, is a highly efficient BCL6 inhibitor that is capable of suppressing the BTB domain of BCL6, with an IC₅₀ value of ≤ 3 nM, exhibiting antitumor activity.

DK-TCIP2, linking inhibitor of CDK9 SNS-032 (HY-10008) with ligands of BCL6 BI-3812 (HY-111381), is a anticancer agent. DK-TCIP2 shows anticancer activity in vivo and in vitro and can be used for study of lymphoma cancer.

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).

WK369 is a novel BCL6 small molecule inhibitor, which exhibits excellent anti-ovarian cancer bioactivity, induces cell cycle arrest and causes apoptosis. WK369 can directly bind to the BCL6-BTB domain and block the interaction between BCL6 and SMRT, leading to the reactivation of p53, ATR and CDKN1A.

CCT374705 is an orally active BCL6 inhibitor (IC₅₀ = 4.8 nM) with potent antiproliferative effects in vitro. CCT374705 effectively inhibits tumor growth in a lymphoma xenograft mouse model.

GSK137 is an orally active, potent and selective B-cell lymphoma 6 (BCL6) inhibitor. GSK137 blocks the interaction between BCL6 and corepressors (e.g., SMRT), reducing the number of germinal center B cells. GSK137 is promising for research of autoimmune diseases such as systemic lupus erythematosus (SLE) and B-cell-related tumors such as diffuse large B-cell lymphoma.

BCL6-IN-11 (Compound 8) is an efficient inhibitor that induces partial degradation of BCL6 with its IC₅₀ value for inhibiting the interaction between BCL6 and its co-inhibitory proteins (such as NCOR1) of 6 nM. BCL6-IN-11 can induce approximately 52% degradation of BCL6 after being treated with 5 μM concentration for 90 minutes, and thus is also classified as a partial degrader. BCL6-IN-11 can be used for the study of lymphoma.

WK692 is a BCL6 inhibitor that inhibits the BCL6^BTB/SMRT interaction. WK692 can effectively inhibit the growth of diffuse large B-cell lymphoma cells and synergize with EZH2 and PRMT5 inhibitors..

JWZ-7-7-Neg1 is a transcriptional chemical inducers of proximity (TCIP) with negative chemical control. JWZ-7-7-Neg1 reduces the ability to bind to BRD4 or BCL6, so it has less cytotoxicity to DLBCL cells, in compared with JWZ-7-7.

BCOR(498-514), biotinylated is the minimal BCL6 binding domain with an K_D value of 1.32 µM. BCOR(498-514), biotinylated blocks BCL6-mediated transcriptional repression and kills lymphoma cells.

BCL6 ligand-2 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). BCL6 ligand-2 can be used for synthesis DZ-837 (HY-161989).

BCL6-IN-12 (Compound 11e) is a BCL6 inhibitor with a K_d of 0.81 μM. BCL6-IN-12 binds to the BTB domain of BCL6. BCL6-IN-12 can be used in the research of diffuse large B-cell lymphoma.

WK500B is a potent and orally active BCL6 inhibitor with a K_D of 1.61 μM. WK500B engages intracellular BCL6 and disrupts BCL6‑corepressor interactions to reactivate BCL6 target genes. WK500B exerts cytotoxicity against diffuse large B‑cell lymphoma cells and induces apoptosis and cell cycle arrest. WK500B suppresses germinal center formation in C57BL/6 mice and DLBCL tumor growth in SCID xenograft models without observable toxicity. WK500B can be used for the study of diffuse large B‑cell lymphoma (DLBCL).

BCL6-IN-10 (Compound 6) is a selective partially degradable molecular glue inhibitor that targets the BTB domain of BCL6 with an IC₅₀ of 4 nM. BCL6-IN-10 shows anti-proliferative effect in diffuse large B-cell lymphoma (DLBCL) cell lines. BCL6-IN-10 can be used for the research of cancer .

IKZF1/3 ligand-1 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC IKZF1/3 Degrader-1 (HY-179075). PROTAC IKZF1/3 Degrader-1 is a potent IKZF1/3 PROTAC degrader with neuroprotective activity.

BCL6 ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). BCL6 ligand-3 can serve as an active control for the target protein ligand of BMS-986458 (HY-172736).

SMRT peptide is one of the co-repressors of BCL6 BTB domain interaction. SMRT peptide binds to the BTB domain of BCL6 and enhances the transcriptional repression function of BCL6. SMRT peptide can be used to study protein-protein interactions.

BCL6-IN-14 is a BCL6 inhibitor with a K_d value of 41.1 μM for the BCL6 BTB domain. BCL6-IN-14 inhibits Karpas-422 tumors. BCL6-IN-14 can be used in cancer-related research.