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Catalog No.
Product Name
Application
Product Information
Citations
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BRD2/BRD4 Inhibitor
KB-0118 is a selective inhibitor of the bromodomains BRD2 and BRD4, exhibiting Kd values of 36.7 μM and 47.4 μM, respectively. This orally active compound effectively inhibits the production of pro-inflammatory cytokines, such as TNF, IL-1β, and IL-23a, and selectively reduces Th17 cell differentiation. The compound modulates Th17-driven inflammatory processes through the epigenetic suppression of BRD4, leading to decreased expression of STAT3 and other target genes. KB-0118 demonstrates potential therapeutic benefits in models of inflammatory bowel disease (IBD). -
BAZ2A Bromodomain Inhibitor
4-Chloro-N-methylpicolinamide is a selective inhibitor of the BAZ2A bromodomain, exhibiting a Kd of over 500 μM. This compound interacts through a weak hydrogen bond with the carbonyl oxygen of Pro1817, offering insights into bromodomain-targeted therapies. It is applicable in the study of invasive prostate cancer, contributing to research focused on cancer biology and therapeutic strategies. -
PB1(5)/SMARCA2/4 Inhibitor
SGC-SMARCA-BRDVIII is a potent and selective inhibitor targeting SMARCA2/4 and PB1(5) with dissociation constants (Kds) of 35 nM, 36 nM, and 13 nM, respectively. This compound also demonstrates inhibitory activity against PB1(2) and PB1(3), with Kds of 3.7 μM and 2.0 μM, respectively. SGC-SMARCA-BRDVIII effectively inhibits adipogenesis in 3T3-L1 murine fibroblasts, making it a valuable tool for research in epigenetics and obesity-related studies. -
BRD4 Inhibitor
Biotinylated-JQ1 is a biotinylated derivative of JQ1 that selectively inhibits BRD4 by binding with high affinity to its bromodomain. This compound exhibits significant anti-proliferative activity in MM1.S multiple myeloma cells, with an EC50 value of 0.4 μM. Biotinylated-JQ1 is suitable for research applications targeting BRD4-mediated pathways in cancer biology and epigenetic regulation studies. -
BET Inhibitor
Trotabresib is a reversible and orally active Bromodomain and Extra-Terminal (BET) inhibitor. It demonstrates significant inhibition of BET proteins, which play a crucial role in regulating gene expression associated with cancer progression. Trotabresib is primarily utilized in research focused on advanced solid tumors, providing insights into potential therapeutic strategies for tackling malignancies driven by aberrant transcriptional regulation. -
BRD4 Inhibitor
MS645 is a bivalent inhibitor targeting the bromodomains of BRD4 with a Ki value of 18.4 nM for BRD4-BD1/BD2. This compound effectively spatially constrains bivalent inhibition, leading to sustained repression of BRD4 transcriptional activity in solid tumor cells. MS645 is suitable for research applications exploring the regulation of gene expression and potential therapeutic strategies in oncology. -
PBRM1 Bromodomain Inhibitor
PBRM1-BD2-IN-5 is a selective inhibitor targeting the bromodomain of the PBRM1 protein, demonstrating Kd values of 1.5 μM for PBRM1-BD2 and 3.9 μM for PBRM1-BD5. It exhibits an IC50 of 0.26 μM for PBRM1-BD2, effectively disrupting the interaction between PBRM1 and acetylated histone peptides within the PBAF complex in cell lysates. This compound is valuable for investigating the role of PBRM1 in cancer biology and may contribute to the development of novel anticancer therapeutics. -
Pan-BD2 BET Inhibitor
GSK973 is a highly selective pan-BD2 bromodomain and extraterminal (BET) inhibitor that targets the second bromodomains of the BET protein family. It exhibits potent inhibitory activity with a pIC50 of 7.8 for BRD4 BD2 and notable selectivity, showing a 1600-fold preference for BRD4 BD2 over BRD4 BD1. Additionally, GSK973 demonstrates efficacy against BRD2 BD2, BRD3 BD2, and BRDT BD2, with pIC50 values ranging from 7.4 to 7.8. This compound is valuable for research applications focused on epigenetic regulation and BET protein functions in various disease models, including cancer. -
BET Inhibitor
PROTAC BRD4 ligand-1 functions as a potent inhibitor of Bromodomain and Extra-Terminal (BET) proteins, targeting the BRD4 protein. This compound is utilized in research applications aimed at investigating BET inhibition and its implications in various cancers and inflammatory diseases. By facilitating the targeted degradation of BRD4, PROTAC BRD4 ligand-1 serves as a valuable tool for studying the role of BET proteins in gene regulation and cellular processes. -
BRD4 BD1 Inhibitor
ZL0590 is a potent, orally bioavailable inhibitor of the bromodomain-containing protein 4 (BRD4) BD1 with an IC50 value of 90 nM for human BRD4 BD1. This compound demonstrates significant anti-inflammatory properties, effectively reducing mucosal inflammation in animal models of inflammatory bowel disease and restoring tissue architecture. ZL0590 is suitable for research applications targeting inflammatory diseases, particularly those associated with the gastrointestinal tract. -
BD2-Selective BET Inhibitor
RVX-297 is a selective bromodomain inhibitor targeting the BD2 domain of BET proteins. This compound demonstrates potent inhibition with IC50 values of 0.08 μM for BRD2, 0.05 μM for BRD3, and 0.02 μM for BRD4 at the BD2 site. RVX-297 effectively suppresses inflammatory gene expression in various immune cell types and shows promise in models of acute inflammation and autoimmune disorders, making it a valuable tool for research in inflammatory diseases. -
BRD7/9 Inhibitor
BRD7-IN-1 is a selective inhibitor of the bromodomain-containing protein 7 (BRD7) and bromodomain-containing protein 9 (BRD9). This compound effectively disrupts BRD7/9 interactions and exhibits notable biological activity with DC50 values of 4.5 nM and 1.8 nM, respectively. BRD7-IN-1 serves as a valuable tool for research focused on understanding the roles of BRD7 and BRD9 in cellular processes and is applicable in studies related to epigenetic regulation and cancer therapy. -
BRD9 Inhibitor
GNE-375 is a highly selective inhibitor of BRD9, exhibiting an IC50 of 5 nM. It demonstrates more than 100-fold selectivity for BRD9 compared to BRD4, TAF1, and CECR2. GNE-375 effectively reduces the binding of BRD9 to chromatin, making it a valuable tool for studies of chromatin regulation and the role of BRD9 in epigenetic modulation. This compound is ideal for research applications involving cancer biology and cellular differentiation pathways. -
BRD4 Inhibitor
BRD4 Inhibitor-20 is a selective inhibitor of bromodomain protein 4 (BRD4), targeting both the BD1 and BD2 domains with IC50 values of 19 nM and 28 nM, respectively. This compound exhibits significant anti-proliferative effects in various cancer cell lines, making it useful for studying the role of BRD4 in oncogenesis. BRD4 Inhibitor-20 is particularly applicable in research focused on colon cancer and other malignancies associated with dysregulated BRD4 activity. -
BRD4 Inhibitor
dBRD4-BD1 is a selective BRD4 inhibitor that effectively induces degradation of the BRD4 protein, exhibiting a DC50 value of 280 nM (Dmax=77%). This compound not only selectively diminishes BRD4 levels but also promotes the upregulation of BRD2 and BRD3 protein levels, making it a valuable tool for studying the role of bromodomain proteins in cellular processes. Its low cytotoxicity profile compared to other BRD4 inhibitors highlights its potential for use in various research applications, including cancer biology and epigenetic regulation studies. -
PLK1/BRD4 Inhibitor
PLK1/BRD4-IN-3 is a selective dual inhibitor targeting bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). This compound effectively inhibits BRD4-BD1, PLK1, and BRDT-BD1, exhibiting IC50 values of 0.059 µM, 0.127 µM, and 0.245 µM, respectively. PLK1/BRD4-IN-3 can be employed in research applications focused on cancer biology, particularly in studies investigating cell proliferation and transcriptional regulation. -
CREB-CBP Complex Inhibitor
Naphthol AS-MX phosphate is an inhibitor of the CREB-CBP transcription factor complex, functioning to disrupt its activity. This compound exhibits significant antitumor effects against lung cancer cells, demonstrating an IC50 value of 3.701 μmol/L for inhibiting cell proliferation, as well as reducing colony formation and anchorage-independent growth in soft agar assays. Naphthol AS-MX phosphate serves as a valuable tool for research on KRAS-mutated lung cancer, particularly in instances characterized by poor chemotherapy resistance and unfavorable prognoses. -
BET Inhibitor
I-BET787 is an orally active inhibitor of bromodomain and extraterminal (BET) proteins, specifically targeting BRD4 with pIC50 values of 7.1 for BD1 and 5.9 for BD2. This compound exhibits anti-inflammatory properties in murine models, making it a valuable tool for studying inflammatory pathways and the role of BET proteins in various diseases. I-BET787 is utilized in research focused on cancer, cardiovascular diseases, and autoimmune disorders. -
PBRM1 Bromodomain Inhibitor
PBRM1-BD2-IN-2 is a selective inhibitor targeting the bromodomain of the polybromo-1 (PBRM1) protein. With a binding affinity characterized by a Kd of 9.3 μM and an IC50 of 1.0 μM, this compound exhibits potent inhibitory activity against PBRM1-BD2. PBRM1-BD2-IN-2 is suitable for research focused on cancer biology and the investigation of epigenetic regulation mechanisms in tumorigenesis. -
BET Inhibitor
Zavabresib is a potent inhibitor of bromodomain and extraterminal domain (BET) proteins. It exhibits significant anticancer activity, particularly in prostate cancer, demonstrated by IC50 values of 0.043 and 0.034 μM against LNCaP and 22Rv1 cell lines, respectively. This compound is a valuable tool for investigating the role of BET inhibition in cancer biology and therapeutic development. -
PLK1/BRD4 Inhibitor
PLK1/BRD4-IN-2 is a dual inhibitor targeting both Polo-like kinase 1 (PLK1) and the bromodomain of BRD4, with an IC50 of 40 nM and 28 nM, respectively. This compound is valuable for research into cancer therapeutics and epigenetic regulation, demonstrating potential in studies focused on cell proliferation and transcriptional control. Its ability to simultaneously inhibit these key oncogenic pathways positions PLK1/BRD4-IN-2 as a crucial tool for advancing cancer research and drug discovery initiatives. -
BET Inhibitor
BET-IN-14 is a potent pan BET inhibitor with an IC50 of 5.35 nM, designed to inhibit bromodomain and extraterminal (BET) proteins. It exhibits significant anti-cancer activity, making it a valuable tool for cancer research. Its application spans various studies investigating the role of BET proteins in tumorigenesis and the development of targeted cancer therapies. -
BET Inhibitor
ET-JQ1-OH is a selective BET inhibitor that specifically targets bromodomain-containing protein 4 (Brd4). This compound serves as an effective ligand in the design and development of PROTACs, facilitating the targeted degradation of Brd4 and enhancing research in epigenetic regulation and cancer biology. Its applications extend to studies investigating the role of BET proteins in various diseases, providing a valuable tool for researchers in drug discovery and therapeutic advancements. -
BRD4 Inhibitor
BRD4 Inhibitor-24 is a selective inhibitor of the bromodomain-containing protein 4 (BRD4). It exhibits significant antitumor activity, demonstrated by IC50 values of 33.7 μM against MCF7 cells and 45.9 μM against K652 cells. This compound is valuable for research exploring the role of BRD4 in cancer biology and therapeutic development. -
BRD4 Inhibitor
TAT-PiET-PROTAC is a BRD4 inhibitor designed as a proteolysis-targeting chimera (PROTAC) that incorporates the cell-penetrating peptide TAT-PiET. This compound effectively reduces the levels of BRD4 and JMJD6, demonstrating significant inhibition of cell proliferation. TAT-PiET-PROTAC is particularly relevant for investigating endocrine resistance in ERα-positive breast cancer cells, making it a valuable tool for cancer research. -
BRD4 Bromodomain Inhibitor
iBRD4-BD1 diTFA is a selective inhibitor of the BRD4 bromodomain, demonstrating potent inhibitory activity with an IC50 of 12 nM. This compound is valuable for research on inflammation and oncology, particularly in studies aimed at understanding the role of BRD4 in gene regulation and cancer progression. Its specificity and efficacy make it a useful tool for exploring therapeutic strategies targeting the BRD4 pathway. -
BRD7/9 Inhibitor
(2S,3R)-LP99 is a highly selective inhibitor of BRD7 and BRD9, exhibiting a KD of 99 nM for BRD9. This compound effectively disrupts the binding of BRD7 and BRD9 to acetylated histones both in vitro and in cellular environments. (2S,3R)-LP99 is instrumental for research into the regulatory roles of BRD7 and BRD9 in pro-inflammatory cytokine secretion, making it a valuable tool for studies investigating inflammation and epigenetic regulation. -
BET Inhibitor
(+) -JQ-1-aldehyde is an aldehyde derivative of the BET inhibitor (+)-JQ1, specifically targeting the BET bromodomains. This compound serves as a crucial precursor for the synthesis of PROTACs, facilitating the targeted degradation of proteins associated with various cancers and other diseases. Its application in chemical biology research advances the understanding of epigenetic regulation and therapeutic development. -
BRD4 Inhibitor
OXFBD04 is a selective inhibitor of BRD4 with an IC50 of 166 nM. This compound acts as a potent ligand for the BET bromodomain, also exhibiting modest affinity for the CREBBP bromodomain. OXFBD04 demonstrates significant anti-cancer activity, making it a valuable tool for research in cancer biology and therapeutic development targeting epigenetic regulation. -
BET Inhibitor
FT001 is a selective inhibitor of bromodomain and extraterminal (BET) proteins. It exhibits significant anti-proliferative activity against MV-4-11 leukemia cells, making it a valuable tool for cancer research. FT001 can facilitate studies aimed at understanding the role of BET proteins in tumorigenesis and exploring potential therapeutic strategies for hematological malignancies. -
BET Bromodomains Inhibitor
I-BET282E is a selective pan-inhibitor of all eight BET bromodomains, effectively targeting BRD2, BRD3, and BRD4 with pIC50 values ranging from 6.4 to 7.7. This compound demonstrates potent inhibition and selectivity over other bromodomain-containing proteins, making it a valuable tool for investigating the role of BET proteins in cellular processes. I-BET282E is suited for research applications in cancer biology and epigenetic regulation. -
BRPF Bromodomain Inhibitor
GSK9311 hydrochloride is a bromodomain inhibitor targeting BRPF proteins, specifically designed as a less active analogue of GSK6853 for use as a negative control in research. It exhibits inhibitory activity against the BRPF bromodomain, with pIC50 values of 6.0 for BRPF1 and 4.3 for BRPF2. This compound is valuable for studies investigating the role of bromodomain interactions in cellular processes and for validating the effects of more potent bromodomain inhibitors. -
BRD4 D1 Inhibitor
BRD4 D1-IN-1 is a selective inhibitor of the BRD4 D1 domain, demonstrating an IC50 of less than 0.092 µM and an affinity of 18 nM. This compound exhibits over 500-fold selectivity for BRD4 D1 compared to BRD2 D1 and BRD4 D2, as determined by isothermal titration calorimetry (ITC). BRD4 D1-IN-1 is primarily used in research related to cancer and inflammatory diseases, providing insights into the role of BRD4 in transcriptional regulation. -
BRD2/3/4 Inhibitor
I-BET151 dihydrochloride is a selective inhibitor of the bromodomain and extraterminal (BET) family, targeting BRD2, BRD3, and BRD4 with pIC50 values of 6.1, 6.3, and 6.6, respectively. This compound effectively disrupts the interaction between BET proteins and acetylated lysines, leading to a reduction in transcriptional activity of key oncogenes. I-BET151 dihydrochloride is primarily utilized in cancer research and studies related to inflammatory diseases, making it a valuable tool for elucidating the role of BET proteins in various biological processes. -
BRD4 Inhibitor
BRD4 Inhibitor-23 is a selective inhibitor targeting Bromodomain-containing protein 4 (BRD4), demonstrating potent inhibition with IC50 values of 6.21 nM for BRD4 BD-1 and 1.44 nM for BRD4 BD-2. This compound is valuable for studying the role of BRD4 in various cellular processes, including transcriptional regulation and cell cycle progression. Its applications extend to research in cancer biology and epigenetic regulation, making it a powerful tool for exploring therapeutic interventions. -
BPTF Bromodomain Inhibitor
(S)-GSK1379725A is a selective inhibitor of the bromodomain and PHD finger containing transcription factor (BPTF) with a Kd of 2.8 μM. This compound demonstrates specificity for BPTF and does not significantly inhibit BRD4 bromodomain. Additionally, (S)-GSK1379725A exhibits antimalarial activity, making it a valuable tool for studying transcriptional regulation and potential therapeutic applications against malaria. -
EP300/CBP Inhibitor
EP300/CBP-IN-2 is a potent inhibitor of the EP300 and CBP histone acetyltransferases, targeting the regulation of gene expression involved in cancer biology. This compound demonstrates significant biological activity in vivo, making it a valuable tool for investigating the role of these targets in tumorigenesis and potential therapeutic interventions. Its applications extend to cancer research, exploring novel strategies for epigenetic modulation in cancer treatment. -
BET Inhibitor
BET-IN-9 is a Bromodomain and Extra-Terminal (BET) protein inhibitor that disrupts the interaction between BET proteins and acetylated lysines. This compound exhibits significant biological activity in blocking transcriptional regulation mediated by BET proteins. BET-IN-9 is utilized in research applications investigating cancer biology, inflammation, and other diseases associated with aberrant gene expression. -
BRD4-BD1 Inhibitor
BRD4-BD1-IN-1 is a selective inhibitor of the BRD4-BD1 interaction, exhibiting an IC50 value of 38.20 μM. This compound disrupts the binding of bromodomain-containing protein 4 to acetylated lysines, thereby modulating transcriptional regulation. It is valuable for research into the role of BRD4 in cancer and other diseases, making it a useful tool for understanding epigenetic mechanisms and developing novel therapeutic strategies. -
BRD4 Inhibitor
BRD4 Inhibitor-31 is a potent inhibitor of the bromodomain-containing protein 4 (BRD4), exhibiting inhibitory constants (Kis) of 0.234 μM and 0.295 μM for BRD4 bromodomains BD1 and BD2, respectively. This compound is utilized in research investigating the roles of BRD4 in inflammatory diseases, cancer progression, and AIDS pathogenesis. Its effectiveness in modulating BRD4 activity makes it a valuable tool for understanding the therapeutic potential in various disease contexts. -
Bromodomain Inhibitor
Bromodomain inhibitor-12 (edisylate) is a selective bromodomain inhibitor that targets bromodomain-containing proteins, which play critical roles in the regulation of gene expression. This compound exhibits significant biological activity in modulating transcriptional processes related to autoimmune and inflammatory diseases. Its application in research can enhance the understanding of pathogenic mechanisms and facilitate the development of novel therapeutic strategies. -
CBP Inhibitor
CBP-IN-1 is a potent inhibitor of the CREB-binding protein (CBP) with an IC50 of 1.5 nM. Additionally, it inhibits CBP BRET and BRD4(1), demonstrating IC50 values of 690 nM and 3100 nM, respectively. CBP-IN-1 is valuable for research applications focused on transcriptional regulation and related signal transduction pathways. Its selective inhibitory profile makes it a useful tool in the study of diseases associated with CBP dysregulation. -
SMARCA2/4 Inhibitor
SMARCA2-IN-8 is a selective inhibitor of the SWI/SNF chromatin remodeling complexes SMARCA2 and SMARCA4, exhibiting potent activity with IC50 values of 5 nM and 6 nM, respectively. This compound effectively inhibits the proliferation of SMARCA2-mutated cancer cells, specifically SKMEL5, with an AAC50 of 5 nM and downregulates SMARCA2-dependent KRT80 gene expression at an AAC50 of 10 nM. SMARCA2-IN-8 demonstrates substantial antitumor efficacy and favorable pharmacokinetic properties in preclinical mouse models, making it a valuable tool for investigating chromatin remodeling in cancer research. -
p300/CBP Inhibitor
KB528 is a selective inhibitor of the histone acetyltransferases p300 and CBP, demonstrating low nM IC50 values against these targets while sparing other members of the KAT family. This compound modulates the IRF4 transcriptional network, leading to decreased expression of key oncogenes such as IRF4, MYC, CAV2, and IGLL5, as well as reduced levels of IKZF3 protein. KB528 has been shown to effectively induce apoptosis in multiple myeloma cells, making it a valuable tool for research in multiple myeloma and related oncological studies. -
Bivalent BET Inhibitor
GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. It demonstrates strong binding affinity to BRD4 and BRDT family members, with Kd values ranging from 0.6 to 28 nM. GXH-II-052 exhibits significant antiproliferative activity and effectively reduces c-Myc expression. This compound is valuable for research in cancer biology and epigenetic modulation. -
PBRM1 Bromodomain Inhibitor
PBRM1-BD2-IN-7 is a selective inhibitor targeting the bromodomain of polybromo-1 (PBRM1). With an IC50 value of 0.29 μM, it demonstrates significant inhibitory activity for PBRM1-BD2. This compound is primarily utilized in cancer research, facilitating studies on the role of PBRM1 in tumorigenesis and therapeutic resistance. -
PI3Kδ/BET Inhibitor
PI3Kδ/BET-IN-1 is a selective inhibitor targeting both PI3Kδ and the bromodomain BRD4-BD1. With an IC50 of 112 nM for PI3Kδ and 19 nM for BRD4-BD1, this compound demonstrates potent antiproliferative effects in diffuse large B-cell lymphoma (DLBCL) cells. Its dual inhibition mechanism makes it a valuable tool for research into cancer biology and therapeutic development. -
Bet Inhibitor
SDR-04 is a highly selective BET inhibitor that targets the BRD4-BD1 domain. It demonstrates potent inhibition of cell proliferation in the MV4;11 cancer cell line, making it a valuable tool for investigating the role of BET proteins in oncogenesis. SDR-04 can be utilized in various research applications aimed at understanding cancer biology and developing novel therapeutic strategies. -
Bivalent BET Inhibitor
NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor with high affinity for BRD4 and BRDT family proteins, exhibiting Kd values of 0.095 nM for BRD4-1, 0.32 nM for BRD4-2, and 5.5 nM for BRDT-2, among others. This compound demonstrates notable antiproliferative activity and effectively reduces c-Myc expression. NC-III-49-1 is valuable for research in cancer biology and therapeutic studies targeting BET-related pathways. -
BRDT-BD2 Inhibitor
CDD-1128 is a potent BRDT-BD2 inhibitor with an IC50 value of 521 nM. This compound is primarily utilized in studies focused on nonhormonal contraceptive agents, offering significant potential for advancing reproductive health research. Its selectivity toward the BRDT-BD2 domain makes it a valuable tool for elucidating the biological pathways involved in spermatogenesis.
