BCL6

CID5721353 is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor).

FX1 is an inhibitor of the transcription factor B cell lymphoma 6 (BCL6) with IC50 value of ~35 μM.

BI-3802 is a highly potent BCL6 degrader, inhibiting the BTB domain of BCL6, with an IC50 of ??3 nM; BI-3802 has antitumor activity.

BI-3812 is potent and efficacious BCL6 inhibitor, inhibiting the BTB domain of BCL6, with an IC50 of ??3 nM; BI-3812 has antitumor activity.

ARV-393 is a potent BCL6 PROTAC degrader that facilitates the ubiquitination and subsequent proteasomal degradation of BCL6. This compound exhibits significant biological activity and is particularly relevant for research focused on advanced non-Hodgkin lymphoma. Its ability to modulate protein levels through targeted degradation makes it a valuable tool for elucidating BCL6-related pathways in cancer biology.

PROTAC BCL6/GSPT1 Degrader-1 is a dual-target PROTAC that effectively degrades both BCL6 and GSPT1 proteins. This compound is associated with the inhibition of cell proliferation, along with the induction of DNA damage, cell cycle arrest, and apoptosis, specifically in diffuse large B-cell lymphoma. It serves as a valuable tool for research into tumor biology, particularly in the context of lymphoma and related malignancies.

MNN-02-155 is a bivalent molecular glue that binds simultaneously to p300/CBP and BCL6. This compound effectively activates the BCL6-target reporter gene, leading to significant induction of cell death. MNN-02-155 is particularly relevant for research into diffuse large B cell lymphomas (DLBCLs), providing insights into potential therapeutic strategies involving BCL6 modulation.

TCIP3 is a bivalent molecular glue that targets p300/CBP and BCL6. By redirecting p300 and CBP, TCIP3 activates programmed cell death genes that are typically suppressed by the oncogenic driver BCL6, making it a valuable tool for investigating diffuse large B cell lymphomas (DLBCLs). Importantly, TCIP3 demonstrates no toxicity to non-transformed tonsillar lymphocytes or fibroblasts, ensuring the safety of experimental applications.

Thalidomide-piperazine-Boc is an E3 ligase ligand-linker conjugate that serves as an intermediate in the synthesis of PROTAC targeting B-cell lymphoma 6 protein (BCL6). This compound plays a significant role in targeted protein degradation, facilitating the selective destruction of BCL6 and aiding in research related to cancer therapeutics. Its application is essential for studies focusing on E3 ligase modulation and PROTAC development in oncology.

3-Fluoro-desmethyl-cabozantinib is a selective ligand for the BCL6 protein, facilitating targeted protein degradation through PROTAC technology. It serves as an essential building block in the development of innovative therapeutics aimed at modulating protein levels for various cancer applications. This compound may enhance research into BCL6-related pathways and assist in the design of more effective treatments.

JWZ-7-7-Neg1 is a transcriptional chemical inducer of proximity (TCIP) designed with negative chemical control. This compound selectively reduces the binding affinity to BRD4 and BCL6, thereby exhibiting decreased cytotoxicity in diffuse large B-cell lymphoma (DLBCL) cells compared to its counterpart, JWZ-7-7. JWZ-7-7-Neg1 serves as a valuable tool in cancer research, particularly for studies focusing on transcriptional regulation and targeted therapies.

WK500B is a potent BCL6 inhibitor that disrupts BCL6-corepressor interactions, leading to the reactivation of BCL6 target genes. With a dissociation constant (KD) of 1.61 μM, it demonstrates significant cytotoxicity against diffuse large B-cell lymphoma (DLBCL) cells, inducing apoptosis and cell cycle arrest. Additionally, WK500B effectively suppresses germinal center formation in C57BL/6 mice and reduces DLBCL tumor growth in SCID xenograft models without noticeable toxicity. This compound is valuable for research in the pathogenesis of DLBCL and potential therapeutic interventions.

BCL6-IN-13 is a potent inhibitor of the B-cell lymphoma 6 (BCL6) protein, demonstrating an IC50 value of 2 nM. This compound disrupts the interaction between BCL6 and its target proteins, leading to the activation of transcription factors involved in cellular growth and differentiation. BCL6-IN-13 is primarily utilized in research focused on B-cell malignancies, autoimmune disorders, and understanding the molecular mechanisms underlying oncology-related transcription regulation.

BMS-986458 is a selective cereblon-based BCL6 degrader that exerts antitumor effects through the targeted degradation of the BCL6 protein. By binding to cereblon and interacting with the BTB domain of BCL6, it modulates key pathways such as cell cycle regulation, antiproliferative signals, and interferon responses, while also enhancing CD20 expression and distribution. BMS-986458 influences follicular helper T cell physiology and reduces circulating tumor DNA levels. Its combination with CD20xCD3 bispecific antibodies has been shown to improve T cell infiltration and expansion in tumors. This compound is applicable in research related to B-cell non-Hodgkin lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, and relapsed/refractory lymphoma.

PROTAC BCL6 Degrader-3 is a selective degrader targeting the BCL6 protein through the proteolysis-targeting chimera (PROTAC) approach. This compound mediates the ubiquitination and subsequent degradation of BCL6, facilitating the modulation of pathways associated with cancer and autoimmune diseases. It serves as a valuable tool for researchers exploring therapeutic strategies aimed at BCL6 inhibition and the underlying mechanisms of related diseases.

CCT374705 is a potent BCL6 inhibitor with an IC50 value of 4.8 nM, demonstrating significant antiproliferative effects in vitro. This compound effectively inhibits tumor growth in lymphoma xenograft mouse models, making it a valuable reagent for investigating BCL6-related pathways in cancer research and potential therapeutic applications.

EB-TCIP is an EWSR1::FLI1 binder that operates by forming a ternary complex with the tagged fusion protein BCL6 and FKBP12F36V. This compound specifically recruits the EWSR1::FLI1 fusion to BCL6-associated DNA regions, leading to chromatin remodeling and the relocalization of transcriptional factors. As a result, EB-TCIP activates the expression of previously repressed BCL6 target genes. It serves as a valuable tool in the exploration of innovative epigenetic therapies for Ewing sarcoma.

BCL6-IN-6 is a selective inhibitor targeting the transcriptional repressor B-cell lymphoma 6 (BCL6). It effectively disrupts the interaction between BCL6 and its corepressors, leading to the reactivation of BCL6 target genes in a dose-dependent manner. This compound is particularly relevant for studies focusing on diffuse large B-cell lymphoma (DLBCL) and related oncogenic pathways.

GSK137 is a potent and selective inhibitor of B-cell lymphoma 6 (BCL6), acting primarily by disrupting the interaction between BCL6 and corepressors such as SMRT. This mechanism results in a reduction of germinal center B cells, making GSK137 a valuable tool for investigating autoimmune diseases, including systemic lupus erythematosus (SLE), and B-cell malignancies, such as diffuse large B-cell lymphoma. Its oral bioactivity aids in the exploration of therapeutic strategies targeting these conditions.

BCL6-IN-11 is a potent BCL6 inhibitor that disrupts the interaction between BCL6 and its co-inhibitory proteins, such as NCOR1, with an IC50 value of 6 nM. This compound induces approximately 52% degradation of BCL6 at a concentration of 5 μM over 90 minutes, classifying it as a partial degrader. BCL6-IN-11 is valuable for research applications in studying lymphoma and the role of BCL6 in oncogenesis.

WK692 is a potent inhibitor of BCL6, specifically targeting the BCL6 BTB/SMRT interaction. This compound demonstrates significant biological activity by effectively inhibiting the growth of diffuse large B-cell lymphoma cells. Furthermore, WK692 has been shown to synergize with EZH2 and PRMT5 inhibitors, making it a valuable tool for research into targeted cancer therapies and the mechanistic understanding of lymphoma progression.

BCL6-760 is an orally active BCL-6 PROTAC degrader that selectively targets and degrades BCL-6 with an EC50 of 0.8 nM, without affecting other CRBN substrates. This compound exhibits notable efficacy in orthotopic xenograft mouse models of OCI-LY-1 tumors. BCL6-760 serves as a valuable tool for investigating diffuse large B-cell lymphoma (DLBCL) and for exploring mechanisms related to BCL-6 signaling pathways in cancer research.

BCL6 PROTAC 1 is a selective proteolysis targeting chimera (PROTAC) that targets B-cell lymphoma 6 (BCL6) for degradation. It exhibits potent inhibitory activity on BCL6 cell reporter assays, with an IC50 value of 8.8 µM. This reagent effectively induces degradation of BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines, making it a valuable tool for tumor-related research applications.

BCL6 ligand-8 is a bifunctional linker designed to target the BCL6 protein for degradation via the PROTAC (Proteolysis Targeting Chimeras) mechanism. This compound plays a crucial role in the synthesis of PROTACs, including the effective BCL6-760, known for its anti-tumor properties. BCL6 ligand-8 is primarily utilized in cancer research to explore therapeutic strategies involving protein degradation pathways.

BCL6-IN-10 is a selective molecular glue inhibitor that targets the BTB domain of BCL6, exhibiting an IC50 of 4 nM. This compound demonstrates significant anti-proliferative activity in diffuse large B-cell lymphoma (DLBCL) cell lines, making it a valuable tool in cancer research. Its unique mechanism of action offers insights into therapeutic strategies for targeting BCL6-associated malignancies.

BCL6 ligand-4 is a selective ligand targeting BCL6, a key regulator of oncogenic transcription. This compound is primarily utilized in the synthesis of PROTACs, enabling targeted protein degradation for therapeutic applications in oncology research. BCL6 ligand-4 provides researchers with essential tools to explore BCL6-related pathways and develop innovative cancer treatments.

SMRT peptide is a BCL6 inhibitor that functions by binding to the BTB domain of BCL6, thereby enhancing its transcriptional repression activity. This compound serves as a valuable tool for studying protein-protein interactions related to BCL6 function in various biological processes. Research applications include investigations into the role of BCL6 in cancer and other diseases where transcriptional regulation is critical.

BCL6 ligand-5 is a selective ligand for the BCL6 protein, involved in transcriptional regulation and oncogenesis. This compound serves as a crucial component for the development of PROTAC-based degraders targeting BCL6, such as PROTAC BCL6 Degrader-2. Additionally, BCL6 ligand-5 has applications in tumor research, contributing to the study of cancer biology and therapeutic strategies.

OICR11029 is a selective inhibitor of BCL6, a transcriptional repressor implicated in various cancers. This compound demonstrates significant efficacy in disrupting BCL6 function, making it a valuable tool for investigating its role in tumorigenesis. OICR11029 is particularly useful for research focused on lymphoma and related hematological malignancies.

EN171 is a covalent ligand that selectively modifies cysteine residues C38 and C96 on the 14-3-3 protein, thereby promoting its interactions with estrogen receptor α (ERα), YAP, and TAZ. This modulation leads to a reduction in transcriptional activity associated with both estrogen signaling and the Hippo pathway. EN171 serves as a molecular glue, enhancing native protein interactions, and acts as a covalent recruiter of 14-3-3 in heterobifunctional applications, facilitating the cytosolic sequestering of nuclear neo-substrates such as BRD4 and BCL6.

Thalidomide-PEG3-amide-C2-COOH is an E3 ligase ligand-linker conjugate designed for the synthesis of proteolysis-targeting chimeras (PROTACs). This compound enables the targeted degradation of proteins via the recruitment of E3 ligases, presenting significant potential for therapeutic applications in oncology and other areas of drug discovery. It serves as a building block for the creation of innovative PROTACs, such as BCL6 PROTAC 1, facilitating advancements in protein modulation research.

(3R,4R)-3-Methyl-4-piperidinol serves as a PROTAC linker, facilitating the targeted degradation of proteins through the proteasome pathway. This compound is essential in the synthesis of innovative PROTAC molecules, such as the BCL6 Degrader-3. Its application in chemical biology aids in studying protein interactions and degradation mechanisms, contributing significantly to drug discovery research.

ALV-05-151-02 is a degrader of BCL6 and BCL6B, effectively reducing endogenous BCL6 levels in SuDHL4 cells and BCL6B levels in KYO1 cells, which exhibit high expression of these targets. This compound serves as a valuable tool for researching hematological malignancies by facilitating the study of the role of BCL6 and BCL6B in various malignancies.

ALV-05-077-01 is a selective degrader of BCL6 and BCL6B proteins. It effectively reduces endogenous BCL6 levels in SuDHL4 cells and BCL6B levels in KYO1 cells, both of which exhibit high expression of these proteins. This compound is useful for investigating the role of BCL6 and BCL6B in hematological malignancies and provides insight into potential therapeutic strategies targeting these proteins.