BCL6 inhibitor

CID5721353 (BCL6 inhibitor) is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor) that disrupts BCL6 corepressor complexes in vitro and in vivo, and was shown to bind the critical site within the BTB groove.

TCIP 1 is a small molecule in the category of transcriptional epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].

BCL6-IN-3 is a potent BCL6 inhibitor with GI50 of 70 nM in SU-DHL4 cells. BCL6-in-3 regulates cell activation, differentiation, DNA damage and apoptosis, and has antitumor activity.

BCL6-IN-8c is an orally active and potent inhibitor of B-cell lymphoma 6 (BCL6)-corepressor interaction(IC50 of 0.10 μM in cell-free enzyme-linked immunosorbent assay).

BI-3812 is an inhibitor of BCL6. Which inhibiting the BTB domain of BCL6 (IC50: 3 nM). BI-3812 also has antitumor activity.

Compound WK692 (compund WK692) is a BCL6 inhibitor that effectively suppresses the growth of diffuse large B-cell lymphoma cells without toxic side effects and acts synergistically with inhibitors of EZH2 and PRMT5.

DK-TCIP2 is an anticancer agent formed by linking the CDK9 inhibitor SNS-032 and the BCL6 inhibitor BI-3812. This compound exhibits anticancer activity both in vivo and in vitro, making it suitable for research in lymphoma.

CDK-TCIP1 is a bivalent molecule that links the CDK9 inhibitor SNS-032 with the BCL6 ligand BI3812. It effectively and specifically kills cells overexpressing BCL6, with an EC50 of 7.7 nM for SUDHL5 cells.

WK500B is a BCL6 inhibitor that binds to BCL6 within cells, obstructing the BCL6 repression complex and reactivating target genes of BCL6, which leads to the death of DLBCL cells and induces apoptosis and cell cycle arrest. In animal models, WK500B inhibits the formation of germinal centers (GC) and the growth of DLBCL tumors without toxic side effects. Moreover, WK500B demonstrates strong efficacy and favorable pharmacokinetic properties, indicating significant development potential.

BCL6-IN-4, a potent inhibitor of B-cell lymphoma 6 (BCL6), exhibits anti-tumor activities with an inhibitory concentration 50 (IC50) value of 97 nM[1].

BCL6-IN-5 is a highly effective inhibitor of BCL6. It exhibits a pIC50 value of 5.82.

Cambinol (SIRT1 2 Inhibitor IV) is a cell-permeable b-naphthol compound that inhibits the NAD-dependent deacetylase activity of SIRT1 2 (IC50: 56 59 μM, respectively) in a substrate-, but not NAD-, competitive manner. Cambinol inhibits SIRT5 deacetylase activity only at much higher concentrations (IC50 >300 μM) and no inhibitory for the class I and II HDACs. In BCL6-expressing Burkitt lymphoma cell lines, Cambinol-induced apoptosis has been attributed to the hyperacetylation of p53 and BCL6.Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

FX1 is an effective and selective BCL6 inhibitor (IC50: 35 μM).

BCL6-IN-6 is an inhibitor of Bcl-6 and can be used in studies about diffuse large B-cell lymphoma. BCL6-IN-6 blocks the interaction of Bcl-6 with its corepressors and dose-dependently reactivates Bcl-6 target genes.

BCL6-IN-9 (compound 1) is a potent inhibitor of B-cell lymphoma 6 protein (BCL6) with an IC50 of 3.9 nM and is utilized for cancer research.

CCT369260 (compound 1), an orally active inhibitor targeting B-cell lymphoma 6 (BCL6), demonstrates anti-tumor efficacy with an IC50 value of 520 nM [1].

TMX-2164, a potent and irreversible inhibitor of B-cell lymphoma 6 (BCL6), demonstrates an IC50 of 152 nM, indicating strong inhibitory efficacy. It exhibits prolonged target engagement and effectively inhibits cell proliferation.

OICR12694 (JNJ-65234637) is an orally active B cell lymphoma 6 (BCL6) inhibitor.

OICR12694 (JNJ-65234637) TFA, an orally active B cell lymphoma 6 (BCL6) inhibitor [1], demonstrates effectiveness in targeting BCL6 pathways.

CCT374705, an orally active BCL6 inhibitor, exhibits potent antiproliferative effects in vitro and effectively inhibits tumor growth in a lymphoma xenograft mouse model [1].

BCL6-IN-10 (Compound WK499) is an inhibitor of BCL6 that disrupts its interaction with the SMRT protein, promoting apoptosis, cell cycle arrest, and DNA damage. It effectively hampers the proliferation of various AML cell lines, with IC50 values of 0.91, 1.63, 1.026, 7.42, 0.87, and 0.85 μM for OCI-AML3, THP1, MOLM13, HL60, KG1, and NB4 cells, respectively [1].

BCL6-IN-7 (BCL6 inhibitor-7) is a BCL6 co-repressor interaction inhibitor with potential anticancer activity. It can be used for studying lymphomas.

F1324 is a potent, high-affinity peptidic inhibitor of B cell lymphoma 6 (BCL6) with an IC50 of 1 nM, exhibiting a binding t1 2 value of 441 s and strong inhibitory activity against BCL6 PPI.

F1324 TFA is a potent, high-affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), exhibiting an IC50 of 1 nM.