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Catalog No.
Product Name
Application
Product Information
Citations
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BRD4 Inhibitor
TAT-PiET is a cell-penetrating peptide that specifically inhibits the extra-terminal (ET) domain of bromodomain-containing protein 4 (BRD4). This reagent demonstrates significant biological activity by reducing levels of both BRD4 and JMJD6, thereby effectively inhibiting cell proliferation. TAT-PiET exhibits resilience against endocrine resistance in estrogen receptor alpha (ERα)-positive breast cancer cells, making it a valuable tool for cancer research, particularly within the context of breast cancer studies. -
BET Inhibitor
DDO-8926 is a potent and selective inhibitor of Bromodomain and Extra-Terminal (BET) proteins, targeting their role in the transcriptional regulation of pro-inflammatory cytokines. This compound has been shown to significantly alleviate mechanical hypersensitivity, making it an important tool for studying neuropathic pain. Its application in research can enhance the understanding of inflammation-related pain mechanisms and provide insights into potential therapeutic strategies. -
BRD7/BRD9 Inhibitor
BRD7-IN-3 is a selective inhibitor targeting bromodomain-containing proteins BRD7 and BRD9, demonstrating IC50 values of 1.6 μM and 2.7 μM, respectively. This compound serves as a valuable tool in cancer research, particularly in studies focused on epigenetic regulation and transcriptional modulation. Its ability to disrupt the interaction between bromodomains and acetylated lysines makes it instrumental for investigations into the role of BRD7 and BRD9 in various disease pathways. -
PBRM1 Bromodomain Inhibitor
PBRM1-BD2-IN-6 is a selective inhibitor of the PBRM1 bromodomain, exhibiting a potent IC50 value of 0.22 μM. This compound demonstrates significant antiproliferative activity and is valuable for investigating PBRM1-dependent cancer mechanisms. Its application in research may aid in the development of targeted therapies for cancers that rely on PBRM1 modulation. -
PBRM1 Bromodomain Inhibitor
PBRM1-BD2-IN-1 is a selective inhibitor targeting the bromodomain of PBRM1, exhibiting significant binding affinity with a Kd of 0.7 μM and an IC50 of 0.2 μM. This compound demonstrates potent inhibitory activity, making it a valuable tool for probing the role of PBRM1 in cancer biology. PBRM1-BD2-IN-1 is suitable for research applications focused on cancer mechanisms and the therapeutic potential of bromodomain inhibition. -
SMARCA2 Inhibitor
DCSM06 is a selective inhibitor of the bromodomain within the SWI/SNF chromatin remodeling complex SMARCA2, demonstrating an IC50 of 9.7 μM. This compound modulates chromatin accessibility and regulation of gene expression, making it a valuable tool for studying the role of SMARCA2 in various biological processes. Its application extends to cancer research and epigenetic regulation, providing insights into potential therapeutic strategies targeting chromatin remodeling pathways. -
BRDT-BD2/BRD4-BD2 Inhibitor
CDD-1349 is a selective inhibitor of the BRDT-BD2 and BRD4-BD2 bromodomains, demonstrating a sixfold selectivity for BRDT-BD2 over BRD4-BD2. With an IC50 value of 22 nM against BRDT, this compound serves as a valuable tool in the exploration of nonhormonal contraceptive agents. Its targeted activity makes it suitable for research focused on reproductive biology and potential contraceptive development. -
BET Inhibitor
BET-IN-13 is a potent inhibitor of Bromodomain and Extraterminal (BET) proteins, with an IC50 value of 1.6 nM. This compound effectively decreases the mRNA expression levels of pro-inflammatory cytokines, including TNF-α, IL-1β, IL-6, and NOS2, demonstrating significant anti-inflammatory activity. BET-IN-13 is valuable for research involving acute liver injury and other inflammatory conditions. -
BRD Inhibitor
CPI703 is a selective bromodomain (BRD) inhibitor that targets the BRD of the 5DBM complex. By binding to specific residues in the first domain, CPI703 disrupts protein-protein interactions, leading to the modulation of cellular processes linked to transcription regulation. This compound is utilized in various research applications, including studies on epigenetic regulation and the development of cancer therapeutics. -
BET Inhibitor
RX-37 is a selective bromodomain and extraterminal (BET) inhibitor that targets BET bromodomain proteins, including BRD2, BRD3, and BRD4, with Ki values ranging from 3.2 to 24.7 nM. This compound demonstrates significant potential in cancer research by modulating gene expression pathways associated with oncogenesis. RX-37 is suitable for studies focused on the role of BET proteins in tumor biology and therapeutic interventions. -
BRD4 Inhibitor
BRD4 Inhibitor-40 primarily targets the bromodomain protein BRD4, inhibiting its binding domains BRD4-BD1 and BRD4-BD2 with IC50 values of 16.1 nM and 142.18 nM, respectively. This compound effectively modulates the expression of c-Myc and p21, resulting in G1 phase cell cycle arrest. Additionally, BRD4 Inhibitor-40 has demonstrated efficacy in inhibiting Pkd1-null renal cystic epithelial cells and blocking renal cyst formation in both Madin-Darby canine kidney and embryonic kidney vesicle models, thus showcasing its potential in renal research applications. -
BRDT-BD2 Inhibitor
CDD-1498 is a selective inhibitor of the bromodomain-containing protein BRDT-BD2, exhibiting an IC50 of 978 nM. This compound demonstrates significant potential for use in research focused on nonhormonal contraceptive agents, providing insights into the modulation of male fertility and reproductive biology. Its potency and specificity make it a valuable tool for investigating the role of BRDT-BD2 in these biological processes. -
CBP Bromodomain Inhibitor
Y08262 is a potent and selective CBP bromodomain inhibitor, demonstrating remarkable specificity with an IC50 value of 73.1 nM. This compound is utilized in research focused on acute myeloid leukemia (AML), offering insights into the role of CBP bromodomain interactions in cancer biology. Its selective inhibition makes it a valuable tool for studying the therapeutic potential of targeting bromodomain-containing proteins in hematological malignancies. -
SMARCA2 Inhibitor
SMARCA2-IN-2 is a specific inhibitor of SMARCA2, demonstrating an IC50 range of 101-500 µM. This compound is relevant for investigations into cancer biology, as it provides insights into the role of SMARCA2 in tumorigenesis. Its ability to selectively modulate SMARCA2 activity makes it a valuable tool for understanding epigenetic regulation in cancer research. -
BRD4 Inhibitor
BRD4 Inhibitor-36 is a selective inhibitor of the BRD4 protein, which is implicated in various cancer pathways. This compound disrupts the interaction between BRD4 and acetylated histones, thereby influencing transcriptional regulation. BRD4 Inhibitor-36 is primarily utilized in cancer research to explore its effects on tumor growth and progression, making it a valuable tool for studies investigating the molecular mechanisms of malignancies. -
BRD4 Inhibitor
BRD4-IN-10 is a selective inhibitor of Bromodomain-containing protein 4 (BRD4), exhibiting an IC50 of 13.5 nM. This compound demonstrates anti-inflammatory and anti-fibrotic activities, making it a valuable tool in studies related to renal fibrosis. It also possesses favorable metabolic stability and pharmacokinetic properties, enhancing its suitability for research applications in exploring BRD4-related pathways and therapeutic interventions. -
BRD4 Inhibitor
Bi-magnolignan is an inhibitor of BRD4, a key regulator involved in the recognition of acetylated lysines on histones and non-histone proteins. This compound has been shown to induce DNA damage and promote apoptosis in cancer cells, specifically inhibiting the proliferation of HCT116 cells with an IC50 value of 2.9 μM. Bi-magnolignan may serve as a valuable tool for elucidating the role of BRD4 in cancer biology and for developing novel therapeutic strategies against BRD4-dependent malignancies. -
BRD4 BrD1 inhibitor
Olinone is a selective inhibitor of the bromodomain-containing proteins BRD4 and BrD1. This compound has been shown to accelerate the differentiation of primary oligodendrocyte progenitors derived from mouse models, making it a valuable tool for studying oligodendrocyte development and associated neural pathways. Its specificity for BRD4 and BrD1 further supports its use in research focusing on epigenetic regulation and potential neurodegenerative disease mechanisms. -
BET Inhibitor
EBET-590 is a potent bromodomain and extraterminal (BET) inhibitor that selectively targets BET proteins, disrupting their interactions with acetylated histones. This compound exhibits significant anti-proliferative activity in various cancer cell lines, making it a valuable tool for cancer research. It is particularly relevant for studies focused on epigenetic regulation and the development of targeted cancer therapies. -
BET Inhibitor
BET-IN-7 is a potent inhibitor of bromodomain and extra-terminal (BET) proteins, exhibiting a Ki value of 12.27 μM and a Kd of 89.3 μM. This compound demonstrates significant potential in research related to sepsis and other inflammatory conditions by modulating transcriptional regulation. Its ability to interfere with BET protein activity makes it a valuable tool for studying epigenetic processes and developing therapeutic strategies against related diseases. -
BET Inhibitor
BET-IN-21 is a selective BET inhibitor targeting the extra terminal domain, demonstrating a Ki of 230 nM. This compound effectively inhibits microglial activation and exhibits therapeutic benefits in models of experimental autoimmune encephalomyelitis. It serves as a valuable tool for research into neuroinflammation and related neurodegenerative disorders. -
BET Bromodomain Inhibitor
BET-IN-18 is a pan-BET bromodomain inhibitor targeting Brd4 and BrdT. It exhibits potent competitive inhibition of the binding of acetylated histone substrates as well as the known BET inhibitor (+)-JQ1, with IC50 values of 1.0 μM and 2.3 μM for Brd4 and BrdT, respectively. This compound is useful for investigating BET bromodomain functions in various biological contexts, particularly in the study of multiple myeloma. -
BRD 4/p38α/BRDT Inhibitor
SB-284851-BT is a selective inhibitor of BRD4, p38α, and BRDT. It effectively inhibits BRD4-BD1 with an IC50 of 1.7 µM, p38α with a Kd of 0.47 nM, and exhibits additional inhibitory activity against BRDT and BRD4 with IC50 values of 18 µM and 3.7 µM, respectively. SB-284851-BT significantly reduces IL-8 production through p38α inhibition and downregulates crucial oncogenic pathways such as c-Myc and NF-κB via BRD4 inhibition. This compound has potential applications in cancer research and therapeutic development targeting cellular signaling pathways. -
BRD4 BD1 Inhibitor
3-Methylcarbostyril is a selective inhibitor of the bromodomain protein BRD4 BD1, exhibiting a pIC50 value of 4.4. This compound has been utilized in research to investigate the role of BRD4 in various cellular processes, including transcription regulation and oncogenic signaling. Its inhibitory activity makes it a valuable tool for studies focused on cancer therapy and epigenetic modulation. -
BRD4 BD1 Inhibitor
ZL0516 is a selective inhibitor of the BRD4 bromodomain 1 (BD1), demonstrating potent activity in modulating epigenetic regulation. It effectively suppresses inflammatory bowel disease (IBD) through inhibition of the BRD4/NF-κB signaling pathway, which plays a critical role in inflammation and immune responses. This compound is primarily utilized in research focusing on the development of therapeutic strategies for IBD and related inflammatory conditions. -
BRDT-BD2 Inhibitor
CDD-1132 is a potent BRDT-BD2 inhibitor with an IC50 of 13 nM, demonstrating significant selectivity for this target. It plays a crucial role in research applications focused on nonhormonal contraceptive agents by interfering with the bromodomain's function. This compound offers potential insights into the development of innovative reproductive health solutions. -
BET Inhibitor
BET-IN-29 is a bromodomain and extraterminal motif (BET) inhibitor that modulates protein-protein interactions involved in gene regulation. It exhibits potent anti-cancer activity by disrupting the function of BET proteins, which play a critical role in cellular proliferation and survival. This compound is applicable in various research areas, including cancer biology, inflammation, metabolic disorders, neurological diseases, and infectious diseases, making it a valuable tool for elucidating underlying mechanisms in these fields. -
BRD4-BD1/2 Inhibitor
BRD4-BD1/2-IN-1 is a potent inhibitor targeting the bromodomain receptor BRD4, exhibiting IC50 values of less than 100 nM for both BRD4 BD-1 and BD-2. This compound plays a crucial role in modulating gene expression through its interactions with chromatin. It is commonly utilized in research applications focused on cancer biology and therapeutic strategies targeting epigenetic regulation. -
BET Inhibitor
BET-IN-15 is a potent bromodomain and extraterminal (BET) inhibitor that targets BRD4 with IC50 values of 0.64 nM and 0.25 nM for BRD4-BD1 and BRD4-BD2, respectively. This compound exhibits significant antiproliferative activity, making it an important tool for studying the role of BET proteins in cancer and other diseases. Researchers can utilize BET-IN-15 in investigations of transcriptional regulation and the therapeutic potential of BET inhibition in oncology. -
BRD4 Inhibitor
BRD4 Inhibitor-17 is a potent BRD4 inhibitor with an IC50 of 0.33 μM. This compound is involved in the regulation of transcription associated with inflammatory responses, cellular proliferation, and cell cycle progression. BRD4 Inhibitor-17 holds potential as a therapeutic agent for counteracting the effects of arsenical compounds in research applications. -
BET Inhibitor
BET-IN-12 is an orally active inhibitor of bromodomain and extra-terminal (BET) proteins, specifically targeting BRD4 with an IC50 of 0.9 nM. This compound demonstrates significant ability to disrupt BET protein interactions with acetylated lysines, thereby influencing gene expression and cellular signaling pathways. BET-IN-12 is utilized in research exploring therapeutic strategies for various cancers and inflammatory diseases, making it a valuable tool for studying the role of BET proteins in these conditions. -
BET Inhibitor
BET-IN-8 is a potent bromodomain and extraterminal (BET) inhibitor, with a Ki value of 0.83 μM and a Kd of 0.571 μM. This compound exhibits significant biological activity by ameliorating lipopolysaccharide (LPS)-induced sepsis in vivo. BET-IN-8 is valuable for research applications focused on understanding the role of BET proteins in inflammatory responses and sepsis pathophysiology. -
SMARCA2 Inhibitor
SMARCA2-IN-1 is a selective inhibitor of the SWI/SNF chromatin remodeling complex, specifically targeting SMARCA2. With an IC50 of greater than 1000 nM in H1299 cell lines, this compound is useful for studying the role of SMARCA2 in chromatin dynamics and epigenetic regulation. It has potential applications in cancer research, particularly in understanding the implications of chromatin remodeling in tumor progression and therapeutic resistance. -
BRD4 Inhibitor
BRD4-IN-8 is a selective inhibitor of the bromodomain-containing protein 4 (BRD4). It modulates gene expression by disrupting the interaction between BRD4 and acetylated histones, leading to the inhibition of transcriptional elongation. This compound has been shown to exhibit anti-cancer activity and is utilized in research investigating the therapeutic potential of targeting the BRD4 pathway in various malignancies. -
BET Inhibitor
Repibresib is a selective Bromodomain and Extra-Terminal (BET) inhibitor that targets BET proteins involved in the regulation of gene expression. This compound exhibits significant antineoplastic activity, making it a valuable tool for cancer research. Its ability to disrupt the interaction between BET proteins and acetylated lysines can be utilized in the study of various malignancies and in the development of novel therapeutic strategies. -
BRD4 Inhibitor
BRD4-IN-4 is a selective inhibitor of the bromodomain-containing protein 4 (BRD4) with an IC50 of 6.83 μM. This compound effectively inhibits the proliferation of MV4-11 cells and induces cell cycle arrest in the G1 phase. BRD4-IN-4 is primarily utilized in research focused on MLL leukemia, providing insights into the therapeutic potential of targeting BRD4 in cancer treatment. -
BET Inhibitor
GSK-340 is a potent BET inhibitor that exhibits high affinity and selectivity for the bromodomain BD2 of BRD4, with a pIC50 value of 7.2. This compound effectively inhibits the release of MCP-1 in lipopolysaccharide-treated PBMCs and whole blood, demonstrating pIC50 values of 7.4 and 6.0, respectively. GSK-340's immunomodulatory properties make it a valuable tool for research applications in inflammation and cancer biology. -
Pan-BRD4-D1-Biased/BRD4-D2 Inhibitor
DW34 is a pan-BRD4-D1 biased inhibitor with concurrent inhibitory activity against BRD4-D2. It demonstrates potent biological activity with an EC50 of 0.14 μM, making it effective in modulating BRD4 pathways. DW34 significantly mitigates liver inflammation induced by lipopolysaccharide (LPS) and acetaminophen (APAP), primarily by reducing chemokine expression and cellular necrosis. This compound is suitable for research applications focused on inflammatory diseases and BRD4-related pathways. -
BRD4 Inhibitor
CN427 is a quinazoline-based compound that selectively inhibits the bromodomain-containing protein 4 (BRD4) with a Kd of 66 nM. This inhibition disrupts the interaction between BRD4 and acetylated histones, which can lead to altered transcriptional regulation. CN427 is primarily applicable in leukemia research, providing insights into epigenetic modulation and potential therapeutic strategies in this malignancy. -
BRD4 BD2 Inhibitor
BRD4-BD1/2-IN-2 is a highly selective inhibitor targeting the BD2 domain of BRD4, demonstrating IC50 values of less than 0.5 nM for BRD4 BD2 and approximately 300 nM for BRD4 BD1. This compound exhibits significant biological activity in modulating BRD4-related pathways, making it a valuable tool for research in oncology and epigenetic regulation. Its potency and specificity support further exploration of BRD4 as a therapeutic target in various diseases. -
BET Inhibitor
BET-IN-10 is a potent BET inhibitor that selectively targets bromodomain and extraterminal (BET) proteins, crucial for regulating gene expression. This compound demonstrates significant anticancer activity, notably inhibiting the growth of MV4-11 leukemia cells with an IC50 value of 26.5 nM. BET-IN-10 is valuable for research applications focused on cancer biology and the mechanistic study of BET-mediated signaling pathways. -
BRD4 Inhibitor
BRD4 Inhibitor-28 is a selective inhibitor of the bromodomain protein BRD4, targeting the BRD4-BD1 and BRD4-BD2 domains with IC50 values of 15 nM and 55 nM, respectively. Additionally, it demonstrates inhibitory effects on BRD2-BD1, BRD3-BD1, and BRDT-BD1, with IC50 values of 19 nM, 25 nM, and 68 nM. This compound exhibits notable anti-melanoma activity, making it valuable for research in cancer therapeutics and epigenetic modulation. -
BET Inhibitor
SJ1461 is a potent BET inhibitor that selectively targets bromodomain-containing proteins BRD2 and BRD4. It demonstrates high affinity with IC50 values of 1.6 nM for BRD2 (BD1), 0.1 nM for BRD2 (BD2), 6.5 nM for BRD4 (BD1), and 0.2 nM for BRD4 (BD2). SJ1461 is utilized in research applications related to cancer, inflammation, and epigenetic regulation, making it a valuable tool for investigating the role of BET proteins in various biological processes. -
BRD4 Inhibitor
Y02224 is a potent inhibitor of the bromodomain-containing protein 4 (BRD4), which plays a critical role in regulating gene expression and cellular proliferation. This compound exhibits significant antiproliferative activity against leukemia cells, highlighting its potential in cancer research. Additionally, Y02224 may be valuable in investigating therapeutic strategies for castration-resistant prostate cancer (CRPC). -
BRD4 D1 Inhibitor
BRD4 D1-IN-2 is a selective inhibitor targeting BRD4 D1, exhibiting a potent IC50 of less than 0.092 µM. With an affinity of 15 nM for BRD4 D1, this compound demonstrates over 500-fold selectivity against both BRD2 D1 and BRD4 D2, as determined by isothermal titration calorimetry (ITC). BRD4 D1-IN-2 is valuable for research applications exploring the role of BRD4 in epigenetic regulation and its implications in cancer and other diseases. -
BRD4 Inhibitor
BRD4-IN-5 is a selective inhibitor of the bromodomain protein BRD4. It demonstrates notable activity with Ki values of 9.7 nM for the first bromodomain (BDI) and 16.1 nM for the second bromodomain (BDII). This compound is valuable for use in cancer research, particularly in studies exploring the role of BRD4 in oncogenic transcriptional regulation and therapeutic interventions. -
BRDT-BD2 Inhibitor
CDD-1154 is an aminopyrimidine analog that functions as a specific inhibitor of the bromodomain testis-specific protein BRDT-BD2, with an IC50 of 139 nM. This compound is primarily utilized in male contraceptive research, providing valuable insights into fertility regulation and the development of novel contraceptive methods. Its selective activity against BRDT-BD2 supports investigations into potential therapeutic applications in reproductive health. -
BRD4 Inhibitor
BRD4 Inhibitor-29 is a selective bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of less than 100 nM. This compound exhibits notable antiproliferative effects against prostate cancer cells, making it a valuable tool for investigating the role of BRD4 in cancer biology and therapeutic applications. It can be utilized in research aimed at understanding the mechanisms of tumorigenesis and developing new treatment strategies for BRD4-dependent cancers. -
CBP Inhibitor
DC-CPin7 is a selective inhibitor of the CREB-binding protein (CBP) bromodomain, demonstrating an IC50 value of 2.5 μM. This compound modulates CBP-mediated signaling pathways, making it relevant for studies involving transcriptional regulation and epigenetic modifications. DC-CPin7 is suitable for research applications focused on cancer biology and other diseases linked to dysregulated gene expression. -
BET Inhibitor
XL-126 is a selective inhibitor of the bromodomain and extraterminal (BET) protein family, specifically targeting BD1 with a Kd of 8.9 nM. This compound demonstrates significant anti-inflammatory properties while preserving platelet function, making it a valuable tool for research into inflammatory disorders and hematological conditions. XL-126 is particularly useful in studies aimed at understanding the role of BET proteins in disease pathways and therapeutics.
