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BCL6-IN-6 is a potent inhibitor of transcriptional repressor B-cell lymphoma 6(BCL6).BCL6-IN-6 significantly blocks the interaction of BCL6 with its corepressors and reactivates BCL6 target genes in a dose-dependent manner. BCL6-IN-6 has the potential for the research of diffuse large B-cell lymphoma (DLBCL) .
BCL6 ligand-5 (Compound 37) is a BCL6 ligand. BCL6 ligand-5 can be used as a ligand for target protein for PROTAC to develop and design degraders for PROTAC BCL6, such as PROTAC BCL6 Degrader-2 (HY-178803). BCL6 ligand-5 can also be used in tumor research .
BCL6 PROTAC 1 is a selective B-cell lymphoma 6(BCL6)PROTAC. BCL6 PROTAC 1 inhibits BCL6 cell reporter with an IC50 value of 8.8 µM. BCL6 PROTAC 1 significantly degrades BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines. BCL6 PROTAC 1 can be used in tumor related research .
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) .
Bcl6 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Bcl6 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Bcl6 Rat Pre-designed siRNA Set A contains three designed siRNAs for Bcl6 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
BCL6 Human Pre-designed siRNA Set A contains three designed siRNAs for BCL6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
BCL6-760 is an orally active BCL-6 PROTAC degrader with an EC50 of 0.8 nM. BCL6-760 only degrades BCL6 and has no effect on other CRBN substrates. BCL6-760 demonstrates significant efficacy in the orthotopic xenograft mouse model of OCI-LY-1 tumors. BCL6-760 can be used in the research of diffuse Large B-cell Lymphoma (DLBCL) (Pink: BCL-6 ligand (HY-179317); Blue: CRBN ligand (HY-179305); Black: Linker) .
BCL6-IN-9 (compound 1) is a potent B-cell lymphoma 6 protein (BCL6) inhibitor, with an IC50 of 3.9 nM. BCL6-IN-9 can be used for the research of cancer .
TP-021 (BCL6-IN-8c), a chemical probe, is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 μM in cell-free enzyme-linked immunosorbent assay .
BCL6B Human Pre-designed siRNA Set A contains three designed siRNAs for BCL6B gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
BCL6-IN-10 (Compound WK499) is a BCL6 inhibitor. BCL6-IN-10 interrupts the binding of BCL6 to SMRT protein. BCL6-IN-10 induces cell apoptosis, cell cycle arrest and DNA damage. BCL6-IN-10 inhibits AML cell proliferation (IC50s: 0.91, 1.63, 1.026, 7.42, 0.87, 0.85μM for OCl-AML3, THP1, MOLM13, HL60, KG1, NB4 cell respectively) .
BI-3802, a chemical probe, is a highly potent BCL6 degrader and inhibits the Bric-à-brac (BTB) domain of BCL6 with an IC50 of ≤3 nM. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1. BI-3802 has antitumor activity .
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 .
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 .
BCOR(498-514), biotinylated is the minimal BCL6 binding domain with an KD value of 1.32 µM. BCOR(498-514), biotinylated blocks BCL6-mediated transcriptional repression and kills lymphoma cells .
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 .
WK692 is a BCL6 inhibitor that inhibits the BCL6BTB/SMRT interaction. WK692 can effectively inhibit the growth of diffuse large B-cell lymphoma cells and synergize with EZH2 and PRMT5 inhibitors. .
CDK-TCIP1 is a bivalent molecule linking CDK9 inhibitor SNS-032 (HY-10008) to BCL6 ligand BI3812 (HY-111381). CDK-TCIP1 potently and specifically kills BCL6-overexpressing cells with EC50 of 7.7 nM for SUDHL5 cells .
ALV-05-077-01 is a BLC6/BLC6B degrader. ALV-05-077-01 depletes endogenous BCL6 levels in SuDHL4 cells (high BCL6 expression) and BCL6B levels in KYO1 cells (high BCL6B expression). ALV-05-077-01 can be used for the study of hematological malignancies .
ALV-05-151-02 is a BLC6/BLC6B degrader. ALV-05-151-02 depletes endogenous BCL6 levels in SuDHL4 cells (high BCL6 expression) and BCL6B levels in KYO1 cells (high BCL6B expression). ALV-05-151-02 can be used for the study of hematological malignancies .
ARV-393 is a potent and orally active BCL6 PROTAC degrader. ARV-393 induces ubiquitination of BCL6 and its subsequent degradation by the proteasome. ARV-393 has the potential for the research of advanced non-hodgkin lymphoma .
F1324 acetate is a potent, high affinity peptidic inhibitor of B cell lymphoma 6(BCL6), with an IC50 of 1 nM. F1324 acetate exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
F1324 is a potent, high affinity peptidic inhibitor of B cell lymphoma 6(BCL6) with an IC50 of 1 nM. F1324 exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
MNN-02-155 is a bivalent molecular glue with with dual binding to p300/CBP and BCL6. MNN-02-155 induces potent activation of the BCL6-target reporter gene and cell death. MNN-02-155 can be used for the study of diffuse large B cell lymphomas (DLBCLs) .
F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6(BCL6), with an IC50 of 1 nM. F1324 TFA exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
BMS-986458 is a highly selective and orally active BCL6 PROTAC degrader. BMS-986458 simultaneously co-opts cereblon (CRBN) and the BCL6 N-terminal BTB domain to catalyze proximity induced degradation of BCL6. BMS-986458 can be used for the study of B-cell Non-Hodgkin's lymphoma (Pink: Target protein ligand (HY-172740); Black: linker (HY-W267161); Blue: E3 ligase ligand (HY-W593794)) .
EB-TCIP (BAK-04-212) is a bivalent molecule comprised of AP1867 (HY-114434) and BI-3812 (HY-111381). EB-TCIP can form a reversible ternary complex between FKBP F36V and BCL6BTB. EB-TCIP recruits FKBP12 F36V-tagged EWS/FLI1 to DNA sites bound by the transcriptional regulator BCL6, leading to rapid expression of BCL6 target genes (eg: SOCS2 and CXCL11). EWS/FLI1 is a fusion transcription factors in Ewing sarcoma. EB-TCIP can be used for research of deregulated transcription in cancer .
CCT373567 is a potent molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.9 nM. CCT373567 exhibits antiproliferative activity .
TCIP3 is a bivalent molecular glue with with dual binding to p300/CBP and BCL6. TCIP3 redirects p300 and CBP to activate programmed cell death genes normally repressed by the oncogenic driver, BCL6. TCIP3 can be used for the study of diffuse large B cell lymphomas (DLBCLs). TCIP3 exhibits no toxicity in non-transformed tonsillar lymphocytes or fibroblasts .
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 .
TMX-2164 is a potent, irreversible B-cell lymphoma 6(BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells .
CCT369260 (compound 1), a chemical probe, is an orally avtive B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity. CCT369260 (compound 1) exhibits an IC50 of 520 nM .
CCT373566 is a potent and orally active molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo .
TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory agent resistance in multiple myeloma (MM) .
Thalidomide-PEG3-amide-C2-COOH is a synthesized E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs, such as BCL6 PROTAC 1 (HY-122829) .
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 .
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 .
DZ-837 (compound 3d) is a PROTAC targeting BCL6 with a DC50 of approximately 600 nM. DZ-837 can induce cell cycle arrest and exert synergistic anticancer effects with Ibrutinib (HY-10997). DZ-837 is composed of PROTAC target protein ligand BCL6 ligand-2 (HY-161990) (red part), E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), and PROTAC Linker (HY-W245803) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione (HY-W924949) [1] .
Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research .
Transcription is the essential first step in the conversion of the genetic information in the DNA into protein and the major point at which gene expression is controlled. Transcription of protein-coding genes is accomplished by the multi-subunit enzyme RNA polymerase II and an ensemble of ancillary proteins, called transcription factors (TFs). Transcription factors play an important role in the long-term regulation of cell growth, differentiation and responses to environmental cues. Deregulated transcription factors contribute to the pathogenesis of a plethora of human diseases, ranging from diabetes, inflammatory disorders and cardiovascular disease to many cancers, and thus these proteins hold great therapeutic potential.
MCE offers a unique collection of 2,023 compounds with validated transcription factor targets modulating properties. MCE transcription factor-targeted compound library is an effective tool for researching transcription factors as drug targets as well as modulation of TFs for different therapeutic applications.
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 .
BCOR(498-514), biotinylated is the minimal BCL6 binding domain with an KD value of 1.32 µM. BCOR(498-514), biotinylated blocks BCL6-mediated transcriptional repression and kills lymphoma cells .
F1324 acetate is a potent, high affinity peptidic inhibitor of B cell lymphoma 6(BCL6), with an IC50 of 1 nM. F1324 acetate exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
F1324 is a potent, high affinity peptidic inhibitor of B cell lymphoma 6(BCL6) with an IC50 of 1 nM. F1324 exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6(BCL6), with an IC50 of 1 nM. F1324 TFA exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
BCL6 is a key transcriptional repressor of germinal centers and regulates multiple biological functions and lineages. It forms a complex with corepressors and histone deacetylase, directly binds to 5'-TTCCTAGAA-3', and inhibits genes involved in differentiation, inflammation, apoptosis and cell cycle control in GC B cells. BCL6 Protein, Human (GST) is the recombinant human-derived BCL6 protein, expressed by E. coli , with N-GST labeled tag.
BCL6 is a key transcriptional repressor of germinal centers and regulates multiple biological functions and lineages. It forms a complex with corepressors and histone deacetylase, directly binds to 5'-TTCCTAGAA-3', and inhibits genes involved in differentiation, inflammation, apoptosis and cell cycle control in GC B cells. BCL6 Protein, Human is the recombinant human-derived BCL6 protein, expressed by E. coli , with tag free.
Bcl6 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Bcl6 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Bcl6 Rat Pre-designed siRNA Set A contains three designed siRNAs for Bcl6 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
BCL6 Human Pre-designed siRNA Set A contains three designed siRNAs for BCL6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
BCL6B Human Pre-designed siRNA Set A contains three designed siRNAs for BCL6B gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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